1. Protein Tyrosine Kinase/RTK Cell Cycle/DNA Damage Autophagy Apoptosis
  2. VEGFR PDGFR IRE1 Mitophagy Autophagy Apoptosis
  3. Sunitinib

Sunitinib  (Synonyms: 舒尼替尼; SU 11248)

目录号: HY-10255A 纯度: 98.96%
COA 产品使用指南

Sunitinib (SU 11248) 是一种多靶点受体酪氨酸激酶抑制剂,抑制 VEGFR2PDGFRβIC50 分别为 80 nM 和 2 nM。Sunitinib 是ATP 竞争性抑制剂,可通过抑制自身磷酸化和随后的 RNase 激活来有效抑制 Ire1α 的磷酸化。

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Sunitinib Chemical Structure

Sunitinib Chemical Structure

CAS No. : 557795-19-4

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10 mM * 1 mL in DMSO ¥715
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Other Forms of Sunitinib:

MCE 顾客使用本产品发表的 58 篇科研文献

WB
RT-PCR
IHC
Cell Viability Assay
IF

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (0-100 μM; 72 h) induces significant cell death in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: J Pharm Anal. 2023 Apr 19.

    Sunitinib (3 μM; 24 h) increases the expression of γ-H2Ax and Temozolomide (TMZ; 10 μM; 24 h) increases the induction of Sunitinib, in T98G cells.

    Sunitinib purchased from MCE. Usage Cited in: Theranostics. 2018 Jul 30;8(15):4262-4278.  [Abstract]

    BV2 cells are pretreated with 0.1% DMSO (Ctrl), JuA (25 µM) or JuA (25 µM) with the indicated antagonist of RTKs (Dovitinib at 1 µM, Gefinitib at 2.5 µM, Sunitinib at 2.5 µM and LDC1267 at 1 µM) for 30 min, followed by administration of Aβ42 (5 μM) for 12 h.

    Sunitinib purchased from MCE. Usage Cited in: EBioMedicine. 2018 Nov;37:344-355.  [Abstract]

    Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Western blot analysis of UCP1 protein expression level in mouse brown adipose.

    Sunitinib purchased from MCE. Usage Cited in: EBioMedicine. 2018 Nov;37:344-355.  [Abstract]

    Sutent (Sunitinib Malate) treatment decreases lipid accumulation in adipose and liver tissues and increases UCP1 expression in brown adipose tissue. Representative images of immunohistochemistry stainining of UCP1 in BAT.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In Caki-1 cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Jul 27;8(56):95116-95134.  [Abstract]

    Abemaciclib causes increased PARP cleavage in RCC. In 786-O cells Abemaciclib exposure results in increased PARP cleavage. This effect is more rapid and pronounced when Abemaciclib is combined with Sunitinib.

    Sunitinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Nov 15;8(67):111110-111118.  [Abstract]

    In cell EC50 determination of CHMFL-KIT-031 with parental Colo320DM (KIT wt) and KIT V559D overexpressed Colo320DM cells.

    Sunitinib purchased from MCE. Usage Cited in: J Med Chem. 2016 Sep 22;59(18):8456-72.  [Abstract]

    Effect of compounds 1 (Imatinib), 2 (Sunitinib), and 35 on cKIT mediated signaling pathways in GIST-T1 and GIST-5R cancer cell lines.

    Sunitinib purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by Western blot (with GAPDH as internal control).

    Sunitinib purchased from MCE. Usage Cited in: Int J Clin Exp Pathol. 2015 Apr 1;8(4):3871-81.  [Abstract]

    The relationship between SOX9 and Raf/MEK/ERK signaling pathway. Co-treatment of si-SOX9-1 and Sorafenib (10uM, 15uM)/Sunitinib (2 uM, 3 uM) significantly decreases expression of MEK1 and its phosphorylated protein (p-MEK1/2, p-ERK1/2) as assayed by RT-PCR (with β-actin as internal control).

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    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Sunitinib (SU 11248) is a multi-targeted receptor tyrosine kinase inhibitor with IC50s of 80 nM and 2 nM for VEGFR2 and PDGFRβ, respectively[1]. Sunitinib, an ATP-competitive inhibitor, effectively inhibits autophosphorylation of Ire1α by inhibiting autophosphorylation and consequent RNase activation[2].

    IC50 & Target[1]

    VEGFR2

    80 nM (IC50)

    PDGFRβ

    2 nM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-375 IC50
    11.58 μM
    Compound: SU-11248
    Cytotoxicity against human A375 cells after 48 hrs by MTT assay
    Cytotoxicity against human A375 cells after 48 hrs by MTT assay
    [PMID: 22483608]
    A-375 IC50
    5400 nM
    Compound: Sunitinib
    Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
    Toxicity against human A375 cells after 72 hrs by cell titer-blue assay
    [PMID: 19654408]
    A-431 IC50
    172.1 nM
    Compound: Sunitinib
    Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    Inhibition of EGFR in human A431 cells compound pretreated for 60 min before EGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    [PMID: 25882519]
    A-431 IC50
    172.1 nM
    Compound: Sunitinib
    Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay
    Inhibition of EGFR in human A431 cells by phosphotyrosine ELISA assay
    [PMID: 24890652]
    A-431 IC50
    172.1 μM
    Compound: 4
    Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA
    Inhibition of EGFR tyrosine kinase activity in EGF-stimulated human A431 cells after 60 mins by ELISA
    [PMID: 22204741]
    A-431 IC50
    172.1 μM
    Compound: Sunitinib
    Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
    Inhibition of EGFR in human A431 cells assessed as inhibition of EGF-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
    [PMID: 23434139]
    A-431 IC50
    172.1 μM
    Compound: SU11248
    Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA
    Inhibition of EGFR in human A431 cells pretreated for 60 mins measured after 1 hr by ELISA
    [PMID: 22739090]
    A-431 IC50
    172.1 μM
    Compound: 4
    Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA
    Inhibition of EGFR phosphorylation in human A431 cells after 10 mins by FLISA
    [PMID: 20403700]
    A-431 IC50
    172.1 μM
    Compound: 4
    Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    Inhibition of EGF-induced EGFR phosphorylation in human A431 cells overexpressing EGFR pretreated for 60 mins prior to EGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    [PMID: 23375090]
    A498 IC50
    1.2 μM
    Compound: Sunitinib
    Antiproliferative activity against human A498 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human A498 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 36332882]
    A498 IC50
    1.25 μM
    Compound: Sunitinib
    Cytotoxicity against human A498 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human A498 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 32947227]
    A498 IC50
    4.3 μM
    Compound: Sunitinib
    Cytotoxicity against human A498 cells after 72 hrs by MTT assay
    Cytotoxicity against human A498 cells after 72 hrs by MTT assay
    [PMID: 23489626]
    A498 IC50
    7981 nM
    Compound: Sunitinib
    Antiproliferative activity against human A498 cells after 48 hrs by MTT assay
    Antiproliferative activity against human A498 cells after 48 hrs by MTT assay
    [PMID: 29057042]
    A549 IC50
    10.14 μM
    Compound: Sunitinib
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue assay
    Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 48 hrs by CellTiter-Blue assay
    [PMID: 32531682]
    A549 IC50
    11 μM
    Compound: Sunitinib
    Antiproliferative activity against human A549 cells incubated for 2 days by MTT assay
    Antiproliferative activity against human A549 cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    A549 IC50
    11 μM
    Compound: Sunitinib
    Antiproliferative activity against human A549 cells by MTT assay
    Antiproliferative activity against human A549 cells by MTT assay
    [PMID: 30502686]
    A549 IC50
    12.35 μM
    Compound: SU-11248
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 22483608]
    A549 IC50
    14.4 μM
    Compound: S
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    A549 IC50
    14.4 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    A549 IC50
    14.4 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 27397498]
    A549 IC50
    18.5 μM
    Compound: 3, SU-11248
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    A549 IC50
    2.44 μM
    Compound: Sunitinib
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTS assay
    [PMID: 27575478]
    A549 IC50
    2.44 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23602441]
    A549 IC50
    22.1 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    A549 IC50
    3.06 μM
    Compound: Sunitinib
    Antiproliferative activity against human Non-small-cell lung cancer A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human Non-small-cell lung cancer A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 32531682]
    A549 IC50
    5.73 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 36970141]
    A549 IC50
    6.61 μM
    Compound: Sunitinib
    Cytotoxicity against Homo sapiens (human) A549 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) A549 cells assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    A549 IC50
    7.93 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human A549 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    A549 IC50
    9.1 μM
    Compound: Sunitinib
    Cytotoxicity against human A549 cells by MTT assay
    Cytotoxicity against human A549 cells by MTT assay
    [PMID: 26920800]
    ACHN IC50
    2.5 μM
    Compound: SUN
    Cytotoxicity against human ACHN cells assessed as inhibition of cell viability after 6 days by MTT assay
    Cytotoxicity against human ACHN cells assessed as inhibition of cell viability after 6 days by MTT assay
    [PMID: 23360104]
    ACHN IC50
    5.7 μM
    Compound: Sunitinib
    Cytotoxicity against human ACHN cells after 72 hrs by MTT assay
    Cytotoxicity against human ACHN cells after 72 hrs by MTT assay
    [PMID: 23489626]
    B16-F10 IC50
    15.35 μM
    Compound: Sunitinib
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against mouse B16-F10 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 36970141]
    BaF3 IC50
    > 10 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 EC50
    > 1000 nM
    Compound: Sunitinib
    Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    Inhibition of human BCR-ABL T315I mutant expressed in mouse BAF3 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay
    [PMID: 27010810]
    BaF3 GI50
    0.002 μM
    Compound: 2
    Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT T670I mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 IC50
    0.0023 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Tel-PDGFRbeta assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    0.006 μM
    Compound: 2
    Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT V559D/V654A double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 GI50
    0.009 μM
    Compound: 2
    Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT V559D mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 GI50
    0.02 μM
    Compound: 2
    Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT V654A mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 GI50
    0.023 μM
    Compound: 2
    Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT L567P mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 IC50
    0.035 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing FLT3-ITD assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    0.053 μM
    Compound: 2
    Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT T670I/V559D double mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 GI50
    0.078 μM
    Compound: 2
    Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 IC50
    0.238 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Tel-KDR-myc1.3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 IC50
    0.297 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing PTC3-RET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    0.51 μM
    Compound: 2
    Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT N822K mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 GI50
    1.01 μM
    Compound: 2
    Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay
    Growth inhibition of mouse BAF3 cells measured after 72 hrs by CCK8 assay
    [PMID: 31250638]
    BaF3 IC50
    1.154 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing NPM-ALK assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 IC50
    1.2 μM
    Compound: SU-11248
    Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting
    Growth inhibition of mouse BA/F3 cells assessed as incorporation of [3H]thymidine incorporation after 72 hrs by liquid scintillation counting
    [PMID: 20117004]
    BaF3 IC50
    1.289 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Tel-IGF-1R assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    1.3 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 GI50
    1.38 μM
    Compound: 2
    Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    Inhibition of Tel-fused cKIT D816V mutant (unknown origin) transfected in mouse BAF3 cells assessed as decrease in cell proliferation after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    BaF3 IC50
    1.469 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing KIT D816V mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 IC50
    1.561 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Tel-FGFR3 assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    1.6 μM
    Compound: 2
    Cytotoxicity mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay
    Cytotoxicity mouse BA/F3 cells assessed as cell growth inhibition after 72 hrs by cell titer-glo assay
    [PMID: 27545040]
    BaF3 GI50
    19.38 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835H mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835H mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 GI50
    2.3 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835V mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835V mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 IC50
    3.846 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing ERBB2 V659E mutant assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    4.3 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835N mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835N mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 GI50
    4.789 μM
    Compound: 2
    Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
    Cytotoxicity in mouse parental BA/F3 cells incubated for 72 hrs by MTS assay
    [PMID: 30204441]
    BaF3 IC50
    5.124 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Trp-MET assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    6.5 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835F mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835F mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 GI50
    6.9 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835Y mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-WT-D835Y mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 GI50
    67.8 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD-F691L mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD-F691L mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BaF3 IC50
    7.177 μM
    Compound: Sunitinib
    Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    Antiproliferative activity against mouse BaF3 cells expressing Bcr-ABL assessed as cell growth inhibition measured after 72 hrs by Alamar Blue assay
    [PMID: 26629594]
    BaF3 GI50
    8.7 nM
    Compound: Sunitinib
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD-D835Y mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    Growth inhibition of mouse BaF3 cells transfected with FLT3-ITD-D835Y mutation assessed as inhibition of cell growth incubated for 72 hrs by MTT assay
    [PMID: 35923716]
    BEAS-2B IC50
    6.09 μM
    Compound: Sunitinib
    Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human BEAS-2B cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 36970141]
    Bel-7402 EC50
    11 μM
    Compound: Sunitinib
    Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay
    Photocytotoxicity against human Bel7402 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay
    [PMID: 26584085]
    Bel-7402 IC50
    2.67 μM
    Compound: Sunitinib
    Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Bel7402 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    BT-474 EC50
    0.9 μM
    Compound: Sunitinib
    Antiproliferative activity against human BT474 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human BT474 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 30996798]
    BT-549 IC50
    15.5 μM
    Compound: S
    Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human BT549 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    BT-549 IC50
    15.5 μM
    Compound: Sunitinib
    Cytotoxicity against human BT549 cells after 48 hrs by MTT assay
    Cytotoxicity against human BT549 cells after 48 hrs by MTT assay
    [PMID: 27397498]
    BT-549 IC50
    15.5 μM
    Compound: Sunitinib
    Cytotoxicity against human BT549 cells after 48 hrs by MTT assay
    Cytotoxicity against human BT549 cells after 48 hrs by MTT assay
    [PMID: 27128173]
    BT-549 IC50
    15.54 μM
    Compound: Sunitinib
    Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human BT549 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    BT-549 IC50
    2.2 μM
    Compound: Sunitinib(R)
    Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay
    Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay
    [PMID: 31699610]
    BT-549 IC50
    3.5 μM
    Compound: Sunitinib(R)
    Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human BT549 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
    [PMID: 31699610]
    BXPC-3 EC50
    > 1000 nM
    Compound: Sunitinib
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    [PMID: 27010810]
    BXPC-3 EC50
    2.5 μM
    Compound: Sunitinib
    Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 30996798]
    BXPC-3 IC50
    3.63 μM
    Compound: 2
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human BxPC3 cells after 72 hrs by MTT assay
    [PMID: 23999040]
    CAKI-1 GI50
    0.63 μM
    Compound: NSC 750690
    Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay
    Antiproliferative activity against human CAKI-1 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    CAKI-1 IC50
    4.93 μM
    Compound: Sunitinib
    Cytotoxicity against human CAKI-1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human CAKI-1 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 32947227]
    CAKI-2 EC50
    > 1000 nM
    Compound: Sunitinib
    Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Caki2 cells after 72 hrs by MTT assay
    [PMID: 27010810]
    CHO GI50
    2.03 μM
    Compound: 2
    Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against CHO cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    CHO IC50
    33.4 μM
    Compound: sunitinib
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    Inhibition of Cav1.2 current measured using QPatch automatic path clamp system in CHO cells expressing Cav1.2, beta-2 and alpha-2/delta-1 subunits
    [PMID: 23812503]
    COLO 205 IC50
    > 4 μM
    Compound: 1a
    Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay
    Antiproliferative activity against human COLO205 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    COLO 205 IC50
    8 μM
    Compound: Sunitinib
    Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay
    Cytotoxicity against human COLO205 cells after 24 hrs by MTT assay
    [PMID: 28756024]
    DU-145 IC50
    16.3 μM
    Compound: S
    Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    DU-145 IC50
    16.38 μM
    Compound: Sunitinib
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human DU145 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    DU-145 IC50
    16.4 μM
    Compound: Sunitinib
    Cytotoxicity against human DU145 cells after 48 hrs by MTT assay
    Cytotoxicity against human DU145 cells after 48 hrs by MTT assay
    [PMID: 27397498]
    DU-145 IC50
    16.4 μM
    Compound: Sunitinib
    Cytotoxicity against human DU145 cells after 48 hrs by MTT assay
    Cytotoxicity against human DU145 cells after 48 hrs by MTT assay
    [PMID: 27128173]
    EKVX GI50
    7.9 μM
    Compound: NSC 750690
    Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay
    Antiproliferative activity against human EKVX cells after 48 hrs by SRB assay
    [PMID: 22560627]
    GIST430 GI50
    2000 nM
    Compound: 2
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining
    [PMID: 31721578]
    GIST430 GI50
    47 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by MTS assay
    [PMID: 30968693]
    GIST430 GI50
    47 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass
    Antiproliferative activity against human GIST430 cells harboring c-KIT exon 11 primary in-frame V560-L576 deletion mutant and exon 13 heterozygous secondary missense V654A mutant assessed as reduction in cell viability by methylene blue staining based ass
    [PMID: 30968693]
    GIST430 GI50
    98 nM
    Compound: 2
    Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    Cytotoxicity against human GIST430 cells harboring KIT V654A mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    [PMID: 28991465]
    GIST48 GI50
    2000 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by MTS assay
    [PMID: 30968693]
    GIST48 GI50
    2000 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as reduction in cell viability by methylene blue staining based assay
    [PMID: 30968693]
    GIST48 GI50
    47 nM
    Compound: 2
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay
    Antiproliferative activity against human GIST48 cells harboring c-KIT exon 11 homozygous primary missense V560D mutant and exon 17 heterozygous secondary D820A mutant assessed as cell growth inhibition after 120 hrs by methylene blue staining based assay
    [PMID: 31721578]
    GIST882 GI50
    0.11 μM
    Compound: 2
    Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against cKIT dependent human GIST882 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    GIST882 GI50
    64 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by MTS assay
    [PMID: 30968693]
    GIST882 GI50
    64 nM
    Compound: 2
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as cell growth inhibition after 144 hrs by methylene blue staining based assay
    [PMID: 31721578]
    GIST882 GI50
    64 nM
    Compound: Sunitinib
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay
    Antiproliferative activity against human GIST882 cells harboring c-KIT exon 13 homozygous primary K642E mutant assessed as reduction in cell viability by methylene blue staining based assay
    [PMID: 30968693]
    GISTT1 GI50
    0.004 μM
    Compound: 2
    Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay
    Inhibition of c-KIT 560 to 578 deletion/T670I mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay
    [PMID: 31250638]
    GISTT1 GI50
    0.011 μM
    Compound: 2
    Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay
    Inhibition of c-KIT 560 to 578 deletion mutant in human GISTT1 cells assessed as growth inhibition after 72 hrs by CCK8 assay
    [PMID: 31250638]
    GISTT1 GI50
    0.041 μM
    Compound: 2
    Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against cKIT dependent human GISTT1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    GISTT1 GI50
    38 nM
    Compound: Sunitinib
    Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay
    Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 deletion mutant assessed as reduction in cell viability by MTS assay
    [PMID: 30968693]
    GISTT1 GI50
    38 nM
    Compound: 2
    Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Antiproliferative activity against human GISTT1 cells harboring heterozygous deletion mutation at C-kit exon 11 assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    [PMID: 31721578]
    GISTT1 GI50
    38 nM
    Compound: Sunitinib
    Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay
    Antiproliferative activity against human GISTT1 cells harboring heterozygous V560-Y578 del mutation assessed as reduction in cell viability by methylene blue staining based assay
    [PMID: 30968693]
    GISTT1 GI50
    40 nM
    Compound: 2
    Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    Cytotoxicity against human GISTT1 cells assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    [PMID: 28991465]
    GISTT1 GI50
    5880 nM
    Compound: 2
    Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    Cytotoxicity against human GISTT1 cells harboring KIT D816E mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    [PMID: 28991465]
    GISTT1 GI50
    90 nM
    Compound: 2
    Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    Cytotoxicity against human GISTT1 cells harboring KIT T670I mutant assessed as cell growth inhibition after 72 hrs by CellTiterGlo assay
    [PMID: 28991465]
    H69AR IC50
    5.8 μM
    Compound: Sunitinib
    Antiproliferative activity against multidrug resistant human NCI-H69AR assessed as inhibition of cell proliferation by MTT assay
    Antiproliferative activity against multidrug resistant human NCI-H69AR assessed as inhibition of cell proliferation by MTT assay
    [PMID: 32531682]
    HCT-116 IC50
    10.69 μM
    Compound: Sunitinib
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human HCT-116 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 36970141]
    HCT-116 IC50
    18.35 μM
    Compound: SU-11248
    Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 22483608]
    HCT-116 IC50
    4.71 μM
    Compound: Sunitinib
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTS assay
    [PMID: 27575478]
    HCT-116 IC50
    4.71 μM
    Compound: Sunitinib
    Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HCT116 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23602441]
    HCT-116 IC50
    5.62 μM
    Compound: Sunitinib
    Growth inhibition of human HCT116 cells after 48 hrs by MTT assay
    Growth inhibition of human HCT116 cells after 48 hrs by MTT assay
    [PMID: 27956344]
    HCT-116 IC50
    5.62 μM
    Compound: Sunitinib
    Antiproliferative activity against human HCT116 cells by MTT assay
    Antiproliferative activity against human HCT116 cells by MTT assay
    [PMID: 30059803]
    HCT-116 IC50
    6.1 μM
    Compound: 3, SU-11248
    Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
    Cytotoxicity against human HCT116 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    HEK293 IC50
    5 μM
    Compound: Sunitinib
    Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
    Antiproliferative activity against HEK293 cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    HEK293 IC50
    5 μM
    Compound: Sunitinib
    Antiproliferative activity against HEK293 cells by MTT assay
    Antiproliferative activity against HEK293 cells by MTT assay
    [PMID: 30502686]
    HEK293 IC50
    6.1 μM
    Compound: Sunitinib
    Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
    Inhibition of human OCT1 expressed in HEK293 cells assessed as decrease in uptake of ASP+ after 2 mins by fluorescence assay
    [PMID: 28230985]
    HeLa EC50
    > 10 μM
    Compound: Sutent
    Toxicity in human HeLa cells assessed as cell cycle arrest at G2M phase by flow cytometry based phenotypic drug discovery based assay
    Toxicity in human HeLa cells assessed as cell cycle arrest at G2M phase by flow cytometry based phenotypic drug discovery based assay
    [PMID: 22409666]
    HeLa IC50
    > 30 μM
    Compound: Sunitinib
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human HeLa cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    HeLa IC50
    10.4 μM
    Compound: S
    Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human HeLa cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    HeLa IC50
    7.8 μM
    Compound: Sunitinib
    Antiproliferative activity against human HeLa cells incubated for 2 days by MTT assay
    Antiproliferative activity against human HeLa cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    HeLa IC50
    7.8 μM
    Compound: Sunitinib
    Antiproliferative activity against human HeLa cells by MTT assay
    Antiproliferative activity against human HeLa cells by MTT assay
    [PMID: 30502686]
    HepG2 IC50
    13.24 μM
    Compound: SU-11248
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 22483608]
    HepG2 IC50
    13.6 μM
    Compound: sunitinib
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 25064347]
    HepG2 IC50
    15.4 μM
    Compound: 3, SU-11248
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    Cytotoxicity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    HepG2 IC50
    16.06 μM
    Compound: Sunitinib
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay
    [PMID: 28057423]
    HepG2 IC50
    16.06 μM
    Compound: Sunitinib
    Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human HepG2 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    HepG2 IC50
    3.81 μM
    Compound: 1a
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    HepG2 IC50
    5.61 μM
    Compound: 2
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay
    [PMID: 23999040]
    HepG2 IC50
    7.78 μM
    Compound: Sunitinib
    Antiproliferative activity against human HepG2 cells by MTT assay
    Antiproliferative activity against human HepG2 cells by MTT assay
    [PMID: 30059803]
    HK-2 IC50
    5.85 μM
    Compound: Sunitinib
    Antiproliferative activity against human HK2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HK2 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    HL-60 GI50
    0.001 μM
    Compound: 2
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against human HL60 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    HL-60 IC50
    15.5 μM
    Compound: 3, SU-11248
    Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
    Cytotoxicity against human HL60 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    HL-60 IC50
    21.5 μM
    Compound: Sunitinib
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human HL60 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    HL-60 IC50
    3.53 μM
    Compound: Sunitinib
    Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) HL60 cells assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    HL-60 IC50
    36.8 nM
    Compound: Sunitinib
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human HL60 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25089810]
    HL-60 IC50
    4.95 μM
    Compound: Sunitinib
    Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay
    Cytotoxicity against human HL60 cells after 72 hrs by CCK-8 assay
    [PMID: 27643639]
    HL-60 IC50
    7 μM
    Compound: Sunitinib
    Antiproliferative activity against human HL60 cells by MTT assay
    Antiproliferative activity against human HL60 cells by MTT assay
    [PMID: 30502686]
    HL-60 IC50
    8.7 μM
    Compound: Sunitinib
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 36332882]
    HMEC-1 IC50
    7 μM
    Compound: Sunitinib
    Antiproliferative activity against HMEC1 cells incubated for 2 days by MTT assay
    Antiproliferative activity against HMEC1 cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    HMEC-1 IC50
    7 μM
    Compound: Sunitinib
    Antiproliferative activity against HMEC1 cells by MTT assay
    Antiproliferative activity against HMEC1 cells by MTT assay
    [PMID: 30502686]
    HMEC-1 IC50
    7 μM
    Compound: Sunitinib
    Antiangiogenic activity against HMEC1 cells after 20 hrs by tube formation assay
    Antiangiogenic activity against HMEC1 cells after 20 hrs by tube formation assay
    [PMID: 30502686]
    HT-29 IC50
    0.33 μM
    Compound: Sunitinib, SU11248
    Cytotoxicity against VEGFR expressing human HT-29 cells after 72 hrs by MTT assay
    Cytotoxicity against VEGFR expressing human HT-29 cells after 72 hrs by MTT assay
    [PMID: 23131541]
    HT-29 IC50
    0.33 μM
    Compound: SU11248
    Antiproliferative activity against human HT-29 cells expressing VEGFR after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells expressing VEGFR after 72 hrs by MTT assay
    [PMID: 22444679]
    HT-29 IC50
    1.3 μM
    Compound: Sunitinib
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    [PMID: 21621880]
    HT-29 IC50
    1.47 μM
    Compound: 2
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 23999040]
    HT-29 GI50
    1.6 μM
    Compound: NSC 750690
    Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
    Antiproliferative activity against human HT-29 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    HT-29 IC50
    1.7 μM
    Compound: Sunitinib
    Cytotoxicity against human HT-29 cells by MTT assay
    Cytotoxicity against human HT-29 cells by MTT assay
    [PMID: 26920800]
    HT-29 IC50
    10.34 μM
    Compound: Sunitinib
    Antiproliferative activity against human HT-29 cells assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay
    Antiproliferative activity against human HT-29 cells assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay
    [PMID: 33340911]
    HT-29 IC50
    3.8 μM
    Compound: Sunitinib
    Antiproliferative activity against human HT-29 cells incubated for 2 days by MTT assay
    Antiproliferative activity against human HT-29 cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    HT-29 IC50
    3.8 μM
    Compound: Sunitinib
    Antiproliferative activity against human HT-29 cells by MTT assay
    Antiproliferative activity against human HT-29 cells by MTT assay
    [PMID: 30502686]
    HT-29 IC50
    4.7 μM
    Compound: Sunitinib
    Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human HT-29 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    Huh-7 CC50
    246 μM
    Compound: Sunitinib
    Cytotoxicity against human HuH7 cells infected with DENV2 New Guinea C by microplate alamar blue assay
    Cytotoxicity against human HuH7 cells infected with DENV2 New Guinea C by microplate alamar blue assay
    [PMID: 31136173]
    Huh-7 IC50
    3.03 μM
    Compound: Sunitinib
    Growth inhibition of human HuH7 cells after 48 hrs by MTT assay
    Growth inhibition of human HuH7 cells after 48 hrs by MTT assay
    [PMID: 27956344]
    Huh-7 IC50
    3.03 μM
    Compound: Sunitinib
    Antiproliferative activity against human HuH7 cells by MTT assay
    Antiproliferative activity against human HuH7 cells by MTT assay
    [PMID: 30059803]
    Huh-7 IC50
    4707 nM
    Compound: Sunitinib
    Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human HuH7 cells after 48 hrs by MTT assay
    [PMID: 29057042]
    HUVEC IC50
    > 3 μM
    Compound: Sunitinib
    Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
    Antiproliferative activity against bFGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
    [PMID: 26629594]
    HUVEC IC50
    0.12 μM
    Compound: Sunitinib
    Inhibition of VEGF-A induced HUVEC cell sprouting after 24 hrs by angiogenesis assay
    Inhibition of VEGF-A induced HUVEC cell sprouting after 24 hrs by angiogenesis assay
    [PMID: 21741249]
    HUVEC IC50
    0.546 μM
    Compound: Sunitinib
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation after 8 hrs by matrigel based inverted microscopic analysis
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation after 8 hrs by matrigel based inverted microscopic analysis
    [PMID: 29057052]
    HUVEC IC50
    0.8 μM
    Compound: Sunitinib
    Antiangiogenic activity in HUVEC assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    Antiangiogenic activity in HUVEC assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay
    [PMID: 27176944]
    HUVEC IC50
    1.5 μM
    Compound: Sunitinib
    Anti-angiogenesis activity in HUVEC assessed as inhibition of VEGF-induced tube formation incubated for 6 hrs by capillary tube formation assay
    Anti-angiogenesis activity in HUVEC assessed as inhibition of VEGF-induced tube formation incubated for 6 hrs by capillary tube formation assay
    [PMID: 32892623]
    HUVEC IC50
    2.1 μM
    Compound: Sunitinib
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation incubated for 6 hrs by capillary tube formation assay
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced capillary tube formation incubated for 6 hrs by capillary tube formation assay
    [PMID: 35294831]
    HUVEC IC50
    2.54 μM
    Compound: Sunitinib
    Antivascular activity against HUVEC assessed as inhibition of tube formation incubated for 6 hrs by inverted microscopy
    Antivascular activity against HUVEC assessed as inhibition of tube formation incubated for 6 hrs by inverted microscopy
    [PMID: 33902285]
    HUVEC IC50
    2.75 μM
    Compound: Sunitinib
    Cytotoxicity against VEGF-stimulated HUVECs assessed as growth inhibition by MTT assay
    Cytotoxicity against VEGF-stimulated HUVECs assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    HUVEC IC50
    2.75 μM
    Compound: Su11248
    Inhibition of VEGF-induced cell proliferation in HUVEC by MTT assay
    Inhibition of VEGF-induced cell proliferation in HUVEC by MTT assay
    [PMID: 21450463]
    HUVEC IC50
    3 μM
    Compound: Sunitinib
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    [PMID: 29482944]
    HUVEC IC50
    3.2 μM
    Compound: Sunitinib
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    [PMID: 30384047]
    HUVEC IC50
    3.63 μM
    Compound: Sunitinib
    Antiangiogenic activity against VEGF-induced HUVEC assessed as inhibition of cell proliferation preincubated for 30 mins followed by VEGF addition measured after 24 hrs by MTT assay
    Antiangiogenic activity against VEGF-induced HUVEC assessed as inhibition of cell proliferation preincubated for 30 mins followed by VEGF addition measured after 24 hrs by MTT assay
    [PMID: 31295714]
    HUVEC IC50
    3.9 μM
    Compound: Sunitinib
    Cytotoxicity against HUVECs assessed as growth inhibition by MTT assay
    Cytotoxicity against HUVECs assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    HUVEC IC50
    4.04 μM
    Compound: Sunitinib
    Cytotoxicity against recombinant Homo sapiens (human) basic FGF-stimulated HUVECs assessed as growth inhibition by MTT assay
    Cytotoxicity against recombinant Homo sapiens (human) basic FGF-stimulated HUVECs assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    HUVEC IC50
    4.04 μM
    Compound: Su11248
    Inhibition of bFGF-induced cell proliferation in HUVEC by MTT assay
    Inhibition of bFGF-induced cell proliferation in HUVEC by MTT assay
    [PMID: 21450463]
    HUVEC IC50
    53 nM
    Compound: SU-11248
    Inhibition of KDR autophosphorylation in HUVEC by Western blot analysis
    Inhibition of KDR autophosphorylation in HUVEC by Western blot analysis
    [PMID: 20833039]
    HUVEC IC50
    6.36 μM
    Compound: Sunitinib
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    Antiproliferative activity against HUVEC after 48 hrs by MTT assay
    [PMID: 29587221]
    HUVEC IC50
    6.37 μM
    Compound: Sunitinib
    Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation in presence of VEGF measured after 24 hrs by CCK8 assay
    Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation in presence of VEGF measured after 24 hrs by CCK8 assay
    [PMID: 33340911]
    HUVEC IC50
    6.46 μM
    Compound: Sunitinib
    Antiangiogenic activity against HUVEC assessed as inhibition of cell proliferation measured after 30 mins by MTT assay
    Antiangiogenic activity against HUVEC assessed as inhibition of cell proliferation measured after 30 mins by MTT assay
    [PMID: 31295714]
    HUVEC EC50
    645 nM
    Compound: SU 011248, Sutent
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced tube formation after 24 hrs by phalloidin-sulforhodamine staining method
    Antiangiogenic activity in HUVEC assessed as inhibition of VEGF-induced tube formation after 24 hrs by phalloidin-sulforhodamine staining method
    [PMID: 23583911]
    HUVEC IC50
    7 nM
    Compound: Sunitinib
    Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
    Antiproliferative activity against VEGF-stimulated HUVEC cells assessed as cell growth inhibition measured after 24 hrs by BrdUrd incorporation based spectrophotometric analysis
    [PMID: 26629594]
    HUVEC IC50
    9.92 μM
    Compound: Sunitinib
    Growth inhibition of HUVEC after 24 hrs in presence of VEGF by MTT assay
    Growth inhibition of HUVEC after 24 hrs in presence of VEGF by MTT assay
    [PMID: 29057052]
    IM-9 IC50
    1.35 μM
    Compound: Sunitinib
    Cytotoxicity against Homo sapiens (human) IM9 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) IM9 cells assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    Jurkat IC50
    > 1 μM
    Compound: SU
    Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity in human Jurkat cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 30742435]
    Jurkat IC50
    8.5 μM
    Compound: Sunitinib
    Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human Jurkat cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    K562 GI50
    1 μM
    Compound: 2
    Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against BCR-ABL dependent human K562 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    K562 EC50
    12.5 μM
    Compound: 6
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 24 hrs by cell-titer glo assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 24 hrs by cell-titer glo assay
    [PMID: 32334266]
    K562 IC50
    14 μM
    Compound: Sunitinib
    Cytotoxicity against human K562 cells after 24 hrs by MTT assay
    Cytotoxicity against human K562 cells after 24 hrs by MTT assay
    [PMID: 28756024]
    K562 IC50
    2.41 μM
    Compound: Sunitinib
    Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) K562 cells assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    K562 IC50
    21.9 μM
    Compound: 3, SU-11248
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    Cytotoxicity against human K562 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    K562 IC50
    5.8 μM
    Compound: Sunitinib
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay
    [PMID: 36332882]
    K562 EC50
    7.03 μM
    Compound: 6
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by celltox-green assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 48 hrs by celltox-green assay
    [PMID: 32334266]
    K562 EC50
    7.23 μM
    Compound: 6
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    Cytotoxicity against human K562 cells assessed as reduction in cell viability incubated for 72 hrs by MTS assay
    [PMID: 32334266]
    Kasumi 1 IC50
    0.016 μM
    Compound: 1a
    Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Kasumi-1 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    Kasumi 1 IC50
    15 nM
    Compound: SU-11248
    Inhibition of c-Kit autophosphorylation in human Kasumi-1 cells by Western blot analysis
    Inhibition of c-Kit autophosphorylation in human Kasumi-1 cells by Western blot analysis
    [PMID: 20833039]
    KB 3-1 IC50
    2.3 μM
    Compound: sunitinib
    Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
    Cytotoxicity against human P-gp-negative KB-3-1 cells after 72 hrs by MTT assay
    [PMID: 19397322]
    KB-V1 IC50
    4.1 μM
    Compound: sunitinib
    Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
    Cytotoxicity against human P-glycoprotein-expressing KBV1 cells after 72 hrs by MTT assay
    [PMID: 19397322]
    KU812 cell line GI50
    1.1 μM
    Compound: 2
    Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against BCR-ABL dependent human KU812 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    L02 IC50
    19.93 μM
    Compound: Sunitinib
    Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay
    Antiproliferative activity against human LO2 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    L02 IC50
    4.62 μM
    Compound: Sunitinib
    Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay
    Cytotoxicity against human L02 cells after 72 hrs by CCK-8 assay
    [PMID: 27643639]
    L02 IC50
    75.6 μM
    Compound: sunitinib
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    Antiproliferative activity against human L02 cells after 48 hrs by MTT assay
    [PMID: 25064347]
    Leukemia cell IC50
    0.03 μM
    Compound: 3, SU-11248
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing wild type FLT3 assessed as cell viability after 72 hrs by luciferase assay
    [PMID: 22221201]
    Leukemia cell IC50
    0.03 μM
    Compound: 3, SU-11248
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-ITD mutation assessed as cell viability after 72 hrs by luciferase assay
    [PMID: 22221201]
    Leukemia cell IC50
    1.1 μM
    Compound: 3, SU-11248
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay
    Cytotoxicity against human primary leukemia cells isolated from acute myeloid leukemia patient expressing FLT3-D835Y mutation assessed as cell viability after 72 hrs by luciferase assay
    [PMID: 22221201]
    LNCaP IC50
    12.61 μM
    Compound: S
    Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human LNCAP cells assessed as decrease in cell viability after 48 hrs by MTT assay
    [PMID: 27210438]
    MCF7 IC50
    0.08 μM
    Compound: Sunitinib
    Antiproliferative activity against human MCF7 cells incubated for 2 days by MTT assay
    Antiproliferative activity against human MCF7 cells incubated for 2 days by MTT assay
    [PMID: 30878834]
    MCF7 IC50
    0.08 μM
    Compound: Sunitinib
    Antiproliferative activity against human MCF7 cells by MTT assay
    Antiproliferative activity against human MCF7 cells by MTT assay
    [PMID: 30502686]
    MCF7 EC50
    0.96 μM
    Compound: Sunitinib
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 30996798]
    MCF7 IC50
    10.5 μM
    Compound: sunitinib
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 25064347]
    MCF7 GI50
    2 μM
    Compound: NSC 750690
    Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    MCF7 IC50
    23.76 μM
    Compound: S
    Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    [PMID: 27210438]
    MCF7 IC50
    23.8 μM
    Compound: Sunitinib
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    MCF7 IC50
    25.41 μM
    Compound: Sunitinib
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay
    [PMID: 28057423]
    MCF7 IC50
    25.41 μM
    Compound: Sunitinib
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human MCF7 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    MCF7 IC50
    6.29 μM
    Compound: Sunitinib
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTS assay
    [PMID: 27575478]
    MCF7 IC50
    6.29 μM
    Compound: Sunitinib
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells assessed as growth inhibition after 72 hrs by MTT assay
    [PMID: 23602441]
    MCF7 IC50
    6.8 μM
    Compound: Sunitinib
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human MCF7 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    MDA-MB-231 EC50
    > 1000 nM
    Compound: Sunitinib
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 27010810]
    MDA-MB-231 IC50
    2.6 μM
    Compound: Sunitinib(R)
    Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 48 hrs by MTT assay
    [PMID: 31699610]
    MDA-MB-231 IC50
    3.7 μM
    Compound: Sunitinib(R)
    Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-231 cells expressing NRP1 assessed as cell viability measured after 72 hrs by MTT assay
    [PMID: 31699610]
    MDA-MB-231 IC50
    3.7 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    [PMID: 21621880]
    MDA-MB-231 IC50
    32 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 24 hrs by MTT assay
    [PMID: 28756024]
    MDA-MB-231 IC50
    4.51 μM
    Compound: Sunitinib
    Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay
    Cytotoxicity against Homo sapiens (human) MDA-MB-231 cells assessed as growth inhibition by MTT assay
    10.1007/s00044-012-0170-3
    MDA-MB-231 IC50
    6 μM
    Compound: Sunitinib
    Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay
    Anticancer activity against human MDA-MB-231 cells after 48 hrs by XTT assay
    [PMID: 28325600]
    MDA-MB-231 IC50
    6.98 μM
    Compound: Sunitinib
    Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 24 hrs by MTT assay
    [PMID: 28760313]
    MDA-MB-231 IC50
    7.4 μM
    Compound: S
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    MDA-MB-231 IC50
    7.4 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 27397498]
    MDA-MB-231 IC50
    7.4 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTT assay
    [PMID: 27128173]
    MDA-MB-231 IC50
    7.44 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    MDA-MB-435 GI50
    2 μM
    Compound: NSC 750690
    Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay
    Antiproliferative activity against human MDA-MB-435 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    MDA-MB-435 IC50
    9.3 μM
    Compound: Sunitinib
    Cytotoxicity against human MDA-MB-435 cells by MTT assay
    Cytotoxicity against human MDA-MB-435 cells by MTT assay
    [PMID: 26920800]
    MEG-01 GI50
    1.2 μM
    Compound: 2
    Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against human BCR-ABL dependent MEG01 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    MKN-45 IC50
    9.25 μM
    Compound: Sunitinib
    Antiproliferative activity against human MKN-45 cells assessed assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay
    Antiproliferative activity against human MKN-45 cells assessed assessed as inhibition of VEGF-induced cell proliferation measured after 24 hrs by CCK8 assay
    [PMID: 33340911]
    MOLM-13 EC50
    14.3 nM
    Compound: 6
    Cytotoxicity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by MTS assay
    Cytotoxicity against human MOLM-13 cells assessed as cell viability measured after 72 hrs by MTS assay
    [PMID: 32334266]
    MOLM-13 IC50
    17.7 nM
    Compound: Sunitinib
    Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MOLM13 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25089810]
    MOLM-13 GI50
    54 nM
    Compound: 2
    Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    Antiproliferative activity against human MOLM13 harboring FLT3-ITD mutant assessed as cell growth inhibition after 72 hrs by CellTiter 96 AQueous One Solution Cell Proliferation assay
    [PMID: 31721578]
    MOLM-13 IC50
    69.6 nM
    Compound: Sunitinib
    Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell Counting Kit-8 assay
    Antiproliferative activity against human MOLM-13 cells incubated for 72 hrs by Cell Counting Kit-8 assay
    [PMID: 33797247]
    MOLM-14 GI50
    0.005 μM
    Compound: 2
    Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against FLT3-ITD dependent human MOLM14 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    MONO-MAC-6 IC50
    5.7 μM
    Compound: Sunitinib
    Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human MONO-MAC-6 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    MV4-11 IC50
    < 0.01 μM
    Compound: Sunitinib
    Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 29935772]
    MV4-11 GI50
    0.001 μM
    Compound: 2
    Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against FLT3-ITD dependent human MV4-11 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    MV4-11 IC50
    0.003 μM
    Compound: Sunitinib
    Antiproliferative activity against human MV411 cells after 48 hrs by MTT assay
    Antiproliferative activity against human MV411 cells after 48 hrs by MTT assay
    [PMID: 24904961]
    MV4-11 IC50
    0.003 μM
    Compound: Sunitinib
    Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay
    Cytotoxicity against FLT3-dependent human MV4-11 cells after 72 hrs by MTT assay
    [PMID: 22452518]
    MV4-11 IC50
    0.009 μM
    Compound: 1a
    Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    MV4-11 IC50
    24.3 nM
    Compound: Sunitinib
    Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human MV4-11 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25089810]
    MV4-11 IC50
    31.5 nM
    Compound: Sunitinib
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Cell Counting Kit-8 assay
    Antiproliferative activity against human MV4-11 cells incubated for 72 hrs by Cell Counting Kit-8 assay
    [PMID: 33797247]
    MV4-11 IC50
    38.5 nM
    Compound: Sunitinib
    Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay
    Antiproliferative activity against human MV4-11 cells harboring FLT3 ITD mutant after 72 hrs by MTS assay
    [PMID: 28038328]
    MV4-11 IC50
    4.3 nM
    Compound: sunitinib
    Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay
    Antiproliferative activity against human MV4-11 cells after 72 hrs by cell titer-blue cell viability assay
    [PMID: 19754199]
    MV4-11 IC50
    4.3 nM
    Compound: Sunitinib
    Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
    Cytotoxicity against human MV4-11 cells after 72 hrs by cell titer-blue assay
    [PMID: 19654408]
    MV4-11 IC50
    54 nM
    Compound: SU
    Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
    Cytotoxicity in human MV4-11 cells assessed as inhibition of cellular viability incubated for 72 hrs by CellTiter-Blue assay
    [PMID: 30742435]
    MV4-11 IC50
    8 nM
    Compound: Sunitinib
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
    Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
    [PMID: 32659083]
    MV4-11 IC50
    9 nM
    Compound: SU-11248
    Cytotoxicity against human MV4-11 cells by MTT assay
    Cytotoxicity against human MV4-11 cells by MTT assay
    [PMID: 20833039]
    NCI-H1299 EC50
    1.54 μM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 30996798]
    NCI-H1975 EC50
    > 1000 nM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    [PMID: 27010810]
    NCI-H3122 IC50
    0.83 μM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H3122 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    NCI-H460 IC50
    > 4 μM
    Compound: 1a
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    NCI-H460 IC50
    2.7 μM
    Compound: Sunitinib
    Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    [PMID: 21621880]
    NCI-H460 IC50
    4.31 μM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    NCI-H526 IC50
    1.01 μM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H526 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H526 cells after 72 hrs by MTT assay
    [PMID: 24904961]
    NCI-H727 IC50
    10120 nM
    Compound: Sunitinib
    Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay
    Antiproliferative activity against human NCI-H727 cells after 48 hrs by MTT assay
    [PMID: 29057042]
    NIH3T3 IC50
    18 nM
    Compound: SU-11248
    Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr
    Inhibitory concentration against human KDR kinase expressed in NIH3T3 cells with 4 uM Biotin-Ahx-AEEEYFFLFA-amide at ambient temperature for 1 hr
    [PMID: 16162008]
    OCI-AML-5 IC50
    14 nM
    Compound: Sunitinib
    Antiproliferative activity against human OCI-AML5 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
    Antiproliferative activity against human OCI-AML5 cells assessed as reduction in cell viability after 48 hrs by Alamar Blue assay
    [PMID: 32659083]
    OVCAR-3 GI50
    3.2 μM
    Compound: NSC 750690
    Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay
    Antiproliferative activity against human OVCAR3 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    PA-1 IC50
    7.97 μM
    Compound: S
    Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human PA1 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    [PMID: 27210438]
    PANC-1 EC50
    13 μM
    Compound: Sunitinib
    Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay
    Photocytotoxicity against human PANC1 cells assessed as cell viability preincubated for 5 hrs with cells followed by UVA-1 irradiation at 3.0 mW/cm'2 for 20 mins measured after 48 hrs by CCK8 assay
    [PMID: 26584085]
    PANC-1 IC50
    14.94 μM
    Compound: Sunitinib
    Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human PANC1 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    PBMC IC50
    46.3 μM
    Compound: Sunitinib
    Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human PBMC cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    PC-3 EC50
    > 1000 nM
    Compound: Sunitinib
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 27010810]
    PC-3 IC50
    12.6 μM
    Compound: S
    Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    PC-3 IC50
    19.6 μM
    Compound: Sunitinib
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 48 hrs by MTT assay
    [PMID: 27448916]
    PC-3 IC50
    19.6 μM
    Compound: Sunitinib
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 27128173]
    PC-3 IC50
    25.1 μM
    Compound: 3, SU-11248
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 48 hrs by MTT assay
    [PMID: 22019188]
    PC-3 IC50
    55.6 μM
    Compound: Sunitinib
    Cytotoxicity against human PC3 cells by MTT assay
    Cytotoxicity against human PC3 cells by MTT assay
    [PMID: 26920800]
    PC-9 IC50
    10.97 μM
    Compound: SU-11248
    Cytotoxicity against human PC9 cells after 48 hrs by MTT assay
    Cytotoxicity against human PC9 cells after 48 hrs by MTT assay
    [PMID: 22483608]
    RCC4 IC50
    4 μM
    Compound: Sunitinib
    Anticancer activity against human RCC4 cells after 48 hrs by XTT assay
    Anticancer activity against human RCC4 cells after 48 hrs by XTT assay
    [PMID: 28325600]
    Rec1 GI50
    0.87 μM
    Compound: 2
    Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against human Rec1 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    RS4-11 IC50
    1 μM
    Compound: 1a
    Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay
    Antiproliferative activity against human RS4:11 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    RS4-11 IC50
    16 nM
    Compound: SU-11248
    Inhibition of FLT3 autophosphorylation in human RS4-11 cells by Western blot analysis
    Inhibition of FLT3 autophosphorylation in human RS4-11 cells by Western blot analysis
    [PMID: 20833039]
    RS4-11 IC50
    34 nM
    Compound: Sunitinib
    Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
    Inhibition of FLT3 ITD mutant autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
    [PMID: 19654408]
    RS4-11 IC50
    9.9 nM
    Compound: Sunitinib
    Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
    Inhibition of FLT3 autophosphorylation in human RS4-11 cells after 2 hrs by electrochemiluminescence assay
    [PMID: 19654408]
    RWPE-1 IC50
    23 μM
    Compound: S
    Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human RWPE1 cells assessed as decrease in cell viability after 48 hrs by MTT assay
    [PMID: 27210438]
    RWPE-1 IC50
    23 μM
    Compound: Sunitinib
    Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay
    Cytotoxicity against human RWPE1 cells after 48 hrs by MTT assay
    [PMID: 27128173]
    RWPE-1 IC50
    25.2 μM
    Compound: S
    Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    Cytotoxicity against human RWPE1 cells assessed as cell growth inhibition after 48 hrs by MTT assay
    [PMID: 27639369]
    SF-539 IC50
    12.2 μM
    Compound: 4
    Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA
    Inhibition of PDGFRbeta tyrosine kinase activity in PDGF-BB-stimulated human SF-539 cells after 60 mins by ELISA
    [PMID: 22204741]
    SF-539 IC50
    12.2 μM
    Compound: 4
    Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA
    Inhibition of PDGFRbeta phosphorylation in human SF539 cells after 10 mins by FLISA
    [PMID: 20403700]
    SF-539 IC50
    83.1 μM
    Compound: Sunitinib
    Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
    Inhibition of PDGFRbeta in human SF539 cells assessed as inhibition of PDGFR-BB-induced tyrosine phosphorylation incubated for 60 mins prior to EGF-activation measured 10 mins by ELISA
    [PMID: 23434139]
    SF-539 IC50
    83.1 μM
    Compound: SU11248
    Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA
    Inhibition of PDGFRbeta in human SF539 cells pretreated for 60 mins measured after 1 hr by ELISA
    [PMID: 22739090]
    SF-539 IC50
    83.1 μM
    Compound: 4
    Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    Inhibition of PDGF-BB-induced PDGFR beta phosphorylation in human SF539 cells overexpressing PDGFR beta pretreated for 60 mins prior to PDGF-BB addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    [PMID: 23375090]
    Sf9 IC50
    3021 nM
    Compound: Sunitinib
    Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3
    Inhibition of ATP-activated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 3
    [PMID: 30968693]
    Sf9 IC50
    31 nM
    Compound: 2
    Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine
    Inhibition of wild type recombinant GST-tagged FLT3 (Y567 to S993 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using Her2 peptide as substrate measured after 4 hrs in presence of ATP by Kinase-Glo Plus reagent-based lumine
    [PMID: 31721578]
    Sf9 IC50
    48 nM
    Compound: 2
    Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of
    Inhibition of recombinant N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) (unknown origin) expressed in baculovirus infected Sf9 insect cells using poly (Glu,Tyr) 4:1 as substrate measured after 150 mins in presence of
    [PMID: 31721578]
    Sf9 IC50
    48 nM
    Compound: Sunitinib
    Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr
    Inhibition of recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation measured after 150 mins in pr
    [PMID: 30968693]
    Sf9 IC50
    80 nM
    Compound: Sunitinib
    Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30
    Inhibition of unactivated recombinant human N-terminal 6x-His-tagged c-KIT (547 to 935 residues)/(694 to 753 residues deletion) expressed in baculovirus infected Sf9 insect cells assessed as decrease in poly (Glu,Tyr) 4:1 phosphorylation incubated for 30
    [PMID: 30968693]
    SH-SY5Y IC50
    83.1 nM
    Compound: Sunitinib
    Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay
    Inhibition of PDGFRbeta in human SH-SY5Y cells by phosphotyrosine ELISA assay
    [PMID: 24890652]
    SK-MEL-28 IC50
    4.13 μM
    Compound: Sunitinib
    Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    Cytotoxicity against human SK-MEL-28 cells assessed as reduction in cell viability measured after 48 hrs by MTT assay
    [PMID: 36970141]
    SK-OV-3 EC50
    1.36 μM
    Compound: Sunitinib
    Antiproliferative activity against human SKOV3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human SKOV3 cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 30996798]
    SK-OV-3 IC50
    9.21 μM
    Compound: Sunitinib
    Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    Cytotoxicity against human SKOV3 cells assessed as inhibition of cell viability after 48 hrs by SRB assay
    [PMID: 26009164]
    SMMC-7721 IC50
    6.47 μM
    Compound: Sunitinib
    Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human SMMC7721 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    [PMID: 21621880]
    SNB-19 GI50
    10 μM
    Compound: NSC 750690
    Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay
    Antiproliferative activity against human SNB19 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    SW-620 GI50
    1.3 μM
    Compound: NSC 750690
    Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay
    Antiproliferative activity against human SW620 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    SW-620 IC50
    6.25 μM
    Compound: Sunitinib
    Growth inhibition of human SW620 cells after 48 hrs by MTT assay
    Growth inhibition of human SW620 cells after 48 hrs by MTT assay
    [PMID: 27956344]
    SW-620 IC50
    6.25 μM
    Compound: Sunitinib
    Antiproliferative activity against human SW620 cells by MTT assay
    Antiproliferative activity against human SW620 cells by MTT assay
    [PMID: 30059803]
    SW982 IC50
    41.2 μM
    Compound: Sunitinib
    Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human SW982 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    T-24 IC50
    2.44 μM
    Compound: 2
    Antiproliferative activity against human T24 cells after 72 hrs by MTT assay
    Antiproliferative activity against human T24 cells after 72 hrs by MTT assay
    [PMID: 23999040]
    THP-1 IC50
    > 1 μM
    Compound: SU
    Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
    Cytotoxicity in human THP1 cells assessed as inhibition of cellular viability after 72 hrs by CellTiter-Glo luminescent assay
    [PMID: 30742435]
    THP-1 IC50
    0.5 μM
    Compound: 1a
    Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human THP1 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    THP-1 IC50
    14.9 μM
    Compound: Sunitinib
    Cytotoxicity against human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human THP1 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    THP-1 IC50
    45.7 nM
    Compound: Sunitinib
    Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
    Cytotoxicity against human THP1 cells assessed as cell viability after 48 hrs by MTT assay
    [PMID: 25089810]
    TK-10 GI50
    6.3 μM
    Compound: NSC 750690
    Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay
    Antiproliferative activity against human TK10 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    TT IC50
    0.04 μM
    Compound: Sunitinib
    Antiproliferative activity against human TT cells pretreated for 72 hrs followed by compound-washout measured after 72 hrs by MTT assay
    Antiproliferative activity against human TT cells pretreated for 72 hrs followed by compound-washout measured after 72 hrs by MTT assay
    [PMID: 24904961]
    U-251 IC50
    18.9 nM
    Compound: Sunitinib
    Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    Inhibition of VEGFR2 in human U251 cells compound pretreated for 60 min before VEGF stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    [PMID: 25882519]
    U-251 IC50
    18.9 nM
    Compound: sunitinib
    Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
    Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA
    [PMID: 24900865]
    U-251 IC50
    18.9 nM
    Compound: Sunitinib
    Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay
    Inhibition of VEGFR2 in human U251 cells by phosphotyrosine ELISA assay
    [PMID: 24890652]
    U-251 IC50
    18.9 μM
    Compound: 4
    Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA
    Inhibition of VEGFR2 tyrosine kinase activity in VEGF-stimulated human U251 cells after 60 mins by ELISA
    [PMID: 22204741]
    U-251 IC50
    18.9 μM
    Compound: Sunitinib
    Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA
    Inhibition of VEGFR2 in human U251 cells assessed as inhibition of VEGF-induced tyrosine phosphorylation incubated for 60 mins prior to VEGF-activation measured 10 mins by ELISA
    [PMID: 23434139]
    U-251 IC50
    18.9 μM
    Compound: SU11248
    Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA
    Inhibition of VEGFR2 in human U251 cells pretreated for 60 mins measured after 1 hr by ELISA
    [PMID: 22739090]
    U-251 IC50
    18.9 μM
    Compound: 4
    Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA
    Inhibition of VEGFR2 phosphorylation in human U251 cells after 10 mins by FLISA
    [PMID: 20403700]
    U-251 IC50
    18.9 μM
    Compound: 4
    Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    Inhibition of VEGF-induced VEGFR2 phosphorylation in human U251 cells overexpressing Flk-1 pretreated for 60 mins prior to VEGF addition measured after 10 mins by phosphotyrosine ELISA cytoblot analysis
    [PMID: 23375090]
    U-251 IC50
    83.1 nM
    Compound: Sunitinib
    Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    Inhibition of PDGFR-beta in human U251 cells compound pretreated for 60 min before PDGF-BB stimulation for 10 mins by phosphotyrosine ELISA cytoblot method
    [PMID: 25882519]
    U-87MG ATCC IC50
    59.75 μM
    Compound: S
    Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 48 hrs by MTT assay
    Cytotoxicity against human U87MG cells assessed as decrease in cell viability after 48 hrs by MTT assay
    [PMID: 27210438]
    U-937 IC50
    > 5 μM
    Compound: 1a
    Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
    Antiproliferative activity against human U937 cells after 72 hrs by MTT assay
    [PMID: 20570526]
    U-937 GI50
    1.7 μM
    Compound: 2
    Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    Antiproliferative activity against human U937 cells assessed as reduction in cell viability after 72 hrs by celltiter-glo/CCK8 assay
    [PMID: 27077705]
    U-937 IC50
    13.7 μM
    Compound: Sunitinib
    Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    Cytotoxicity against human U937 cells assessed as reduction in cell viability incubated for 24 hrs by CellTiter-Glo luminescent cell viability assay
    [PMID: 31563013]
    UACC-257 GI50
    4 μM
    Compound: NSC 750690
    Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay
    Antiproliferative activity against human UACC257 cells after 48 hrs by SRB assay
    [PMID: 22560627]
    WI-38 IC50
    8.56 μM
    Compound: Sunitinib
    Cytotoxicity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    Cytotoxicity against human WI38 cells assessed as cell growth inhibition after 72 hrs by MTT assay
    [PMID: 21621880]
    体外研究
    (In Vitro)

    Sunitinib Malate 也是 KIT 和 FLT-3 的良好抑制剂[1]。在 RS4;11 细胞 (FLT3-WT) 中,用 Sunitinib (SU11248) 治疗以剂量依赖性方式抑制 FLT3-WT 磷酸化,IC50 约为 250 nM。在表达 FLT3-ITD 的 MV4;11 细胞中,Sunitinib 以剂量依赖性方式抑制 FLT3-ITD 磷酸化,2 小时治疗后的 IC50 为 50 nM[3]。在生化测定中,Sunitinib 对 Flk-1PDGFRβ 表现出竞争性抑制(就 ATP 而言),Ki 值分别为 9 nM 和 8 nM。Sunitinib 也是一种竞争性 FGFR1 酪氨酸激酶活性抑制剂,尽管效力较低,其 Ki 值为 0.83 μM。除了这三种结构相关的分裂激酶结构域 RTK 外,Sunitinib 的活性还针对一系列其他酪氨酸和丝氨酸/苏氨酸激酶进行了评估。在这些生化测定中,Sunitinib 的 IC50 值通常比 Flk-1PDGFR 的 IC50 值至少高 10 倍(例如,IC50值为:EGFR 和 Cdk2 >10 μM;Met 为 4 μM;IGFR-1 为 2.4 μM;Abl 为 0.8 μM;Src 为 0.6 μM)[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    体内研究
    (In Vivo)

    Sunitinib Malate 口服生物利用度极高,对多种临床前肿瘤模型均有高效治疗作用,有效剂量下耐受性良好[1]。Sunitinib (80 mg/kg/天) 可抑制无胸腺小鼠体内已建立的 SF763T 和 Colo205 肿瘤异种移植瘤的生长。Sunitinib 治疗可有效抑制已建立的肿瘤异种移植瘤的生长[4]

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Clinical Trial
    分子量

    398.47

    Formula

    C22H27FN4O2

    CAS 号
    性状

    固体

    颜色

    Yellow to orange

    中文名称

    舒尼替尼;苏尼替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式

    4°C, protect from light

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 20.83 mg/mL (52.27 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响,请使用新开封的 DMSO)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.5096 mL 12.5480 mL 25.0960 mL
    5 mM 0.5019 mL 2.5096 mL 5.0192 mL
    查看完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    • 摩尔计算器

    • 稀释计算器

    Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

    质量
    =
    浓度
    ×
    体积
    ×
    分子量 *

    Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

    This equation is commonly abbreviated as: C1V1 = C2V2

    浓度 (start)

    C1

    ×
    体积 (start)

    V1

    =
    浓度 (final)

    C2

    ×
    体积 (final)

    V2

    动物实验:

    请根据您的 实验动物和给药方式 选择适当的溶解方案。

    以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:
    ——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用
    以下溶剂前显示的百分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

    • 方案 一

      请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 1.11 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 1.11 mg/mL(饱和度未知)的澄清溶液。

      1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

      生理盐水的配制:将 0.9 g 氯化钠,溶解于 ddH₂O 并定容至 100 mL,可以得到澄清透明的生理盐水溶液。
    • 方案 二

      请依序添加每种溶剂: 10% DMSO    90% Corn Oil

      Solubility: ≥ 1.11 mg/mL (2.79 mM); 澄清溶液

      此方案可获得 ≥ 1.11 mg/mL(饱和度未知)的澄清溶液,此方案实验周期在半个月以上的动物实验酌情使用。

      1 mL 工作液为例,取 100 μL 11.1 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    动物溶解方案计算器
    请输入动物实验的基本信息:

    给药剂量

    mg/kg

    动物的平均体重

    g

    每只动物的给药体积

    μL

    动物数量

    由于实验过程有损耗,建议您多配一只动物的量
    请输入您的动物体内配方组成:
    %
    DMSO +
    +
    %
    Tween-80 +
    %
    Saline
    如果您的动物是免疫缺陷鼠或者体弱鼠,建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。
    方案所需 助溶剂 包括:DMSO ,均可在 MCE 网站选购。 Tween 80,均可在 MCE 网站选购。
    计算结果
    工作液所需浓度 : mg/mL
    储备液配制方法 : mg 药物溶于 μL  DMSO(母液浓度为 mg/mL)。

    *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

    您所需的储备液浓度超过该产品的实测溶解度,以下方案仅供参考,如有需要,请与 MCE 中国技术支持联系。
    动物实验体内工作液的配制方法 : 取 μL DMSO 储备液,加入 μL  μL ,混合均匀至澄清,再加 μL Tween 80,混合均匀至澄清,再加 μL 生理盐水
    连续给药周期超过半月以上,请谨慎选择该方案。
    请确保第一步储备液溶解至澄清状态,从左到右依次添加助溶剂。您可采用超声加热 (超声清洗仪,建议频次 20-40 kHz),涡旋吹打等方式辅助溶解。
    纯度 & 产品资料

    纯度: 98.96%

    参考文献
    Cell Assay
    [3]

    RS4;11 and MV4;11 cell lines are starved overnight in medium containing 0.1% FBS prior to addition of Sunitinib (1 nM, 5 nM, 10 nM, 25 nM, 75 nM, 100 nM, 250 nM, 500 nM) and FL (50 ng/mL; FLT3-WT cells only). Proliferation is measured after 48 hours of culture using the Alamar Blue assay in triplicate for each condition, as described by the manufacturer. Trypan blue cell viability assays are performed in parallel and yielded similar results[3].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [2][4]

    Mice[2]
    Female nu/nu mice (8-12 weeks old, 25 grams) are used. Briefly, 3-5×106 tumor cells are implanted s.c. into the hind flank region of mice on day 0. Daily treatment of tumor-bearing mice with oral administration of Sunitinib as a carboxymethyl cellulose suspension or as a citrate buffered (pH 3.5) solution is initiated once the tumors reached the indicated average size. Tumor growth is evaluated based on twice-weekly measurement of tumor volume. Typically, studies are terminated when tumors in vehicle-treated animals reach an average size of 1000 mm3 or when the tumors are judged to adversely effect the well being of the animals.
    Rats[4]
    Adult male Wistar rats (325-349 g) are used. To validate the ability of the time-lapse imaging method to evaluate the anti-angiogenic effects for a given drug treatment, two drug studies are conducted. In the first study, mesenteric windows are harvested from adult male Wistar rats and cultured for 3 days according to the two experimental groups: 1) 10% serum (n=8 tissues from 4 rats), and 2) 10% serum+Sunitinib (5 μM; n=8 tissues from 4 rats).

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month (protect from light)。-80°C储存时,请在6个月内使用,-20°C储存时,请在1个月内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.5096 mL 12.5480 mL 25.0960 mL 62.7400 mL
    5 mM 0.5019 mL 2.5096 mL 5.0192 mL 12.5480 mL
    10 mM 0.2510 mL 1.2548 mL 2.5096 mL 6.2740 mL
    15 mM 0.1673 mL 0.8365 mL 1.6731 mL 4.1827 mL
    20 mM 0.1255 mL 0.6274 mL 1.2548 mL 3.1370 mL
    25 mM 0.1004 mL 0.5019 mL 1.0038 mL 2.5096 mL
    30 mM 0.0837 mL 0.4183 mL 0.8365 mL 2.0913 mL
    40 mM 0.0627 mL 0.3137 mL 0.6274 mL 1.5685 mL
    50 mM 0.0502 mL 0.2510 mL 0.5019 mL 1.2548 mL
    Help & FAQs
    • Do most proteins show cross-species activity?

      Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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    产品名称:
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    目录号:
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