1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. Osimertinib

Osimertinib  (Synonyms: 奥希替尼; AZD-9291; Mereletinib)

目录号: HY-15772 纯度: 99.96%
COA 产品使用指南

Osimtinib (AZD9291) 是一种共价结合、具有口服活性、不可逆和突变选择性的 EGFR 抑制剂,其有效抑制 L858R (IC50=12 nM) 和 L858R/T790M (IC50=1 nM) EGFR。Osimtinib 解决了肺癌 T790M 突变介导的 EGFR 抑制剂耐药。

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Osimertinib Chemical Structure

Osimertinib Chemical Structure

CAS No. : 1421373-65-0

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Customer Review

Other Forms of Osimertinib:

MCE 顾客使用本产品发表的 107 篇科研文献

Proliferation Assay
WB

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are exposed to indicated concentrations of AZD9291 for 24 h and then stimulated with EGF (100 ng/mL) for 30 min. Cell lysates are prepared and examined using Western blot analysis with indicated antibodies.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    Measurement of antiproliferation effects of AZD9291 by EdU incorporation assay.

    Osimertinib purchased from MCE. Usage Cited in: J Exp Clin Cancer Res. 2019 May 23;38(1):219.   [Abstract]

    U87 and U251 cells are treated with AZD9291 or CP-358774 for 4, 24 and 48 h. The expression level of p-ERK are assessed using Western blot analysis.

    Osimertinib purchased from MCE. Usage Cited in: Acta Pharmacol Sin. 2019 Dec;40(12):1587-1595.  [Abstract]

    MDAMB-453 cells are pre-treated with 10 μM MG132 for 1 h before treatment with the 20 μM AZD for 4 h. Cell lysates were used for SDS PAGE and Western blotting. AZD9291 disrupts the EZH2–EED interaction by binding to EZH2 directly

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of p-EGFR(Tyr1068), p-EGFR(Tyr1137), EGFR, p-STAT3, STAT3, p-AKT, AKT, p-p38 MAPK, and p-ERK MAPK are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Environ Toxicol. 2019 Apr;34(4):476-485.  [Abstract]

    Protein levels of NF-κB and IκB are analyzed are analyzed in GST-Der pII1-129-stimulated human epithelial cells with/without AZD-9291 treatment.

    Osimertinib purchased from MCE. Usage Cited in: Cell Chem Biol. 2018 Aug 16;25(8):996-1005.e4.  [Abstract]

    Negligible increases in caspase-3 activity or PARP-1 cleavage is observed in H1975 NSCLC cells treated with DMSO, single agent PAC-1 (5 mM), or Osimertinib (Osi). In cells treated with PAC-1+Osimertinib, dramatic increases in caspase-3 activity is observed as early as 36 hr post treatment.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2017 Mar 14;8(11):18359-18372.  [Abstract]

    In all of the cell lines tested, AZD9291 significantly affects the phosphorylation of eIF4E, which presumably is due to its strong inhibitory activity against MNK2 kinase.

    Osimertinib purchased from MCE. Usage Cited in: Oncotarget. 2015 Oct 13;6(31):31313-22.  [Abstract]

    Effect of PCI-32765, WZ4002, AZD9291 and CO1686 on EGFR phosphorylation of tyrosines 1068 and 1173 in EGFR-dependent cancer cell lines.
    • 生物活性

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Osimertinib (AZD9291) is a covalent, orally active, irreversible, and mutant-selective EGFR inhibitor with an apparent IC50 of 12 nM against L858R and 1 nM against L858R/T790M, respectively. Osimertinib overcomes T790M-mediated resistance to EGFR inhibitors in lung cancer[1].

    IC50 & Target[1]

    EGFRL858R

    12 nM (IC50, Enzyme assays)

    EGFRL858R/T790M

    1 nM (IC50, Enzyme assays)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A-431 IC50
    0.4 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
    Antiproliferative activity against human A431 wild type cells measured after 72 hrs by Sulforhodamine B assay
    [PMID: 31889606]
    A-431 GI50
    0.596 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    A-431 IC50
    0.61 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    A-431 EC50
    0.67 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human A431 cells expressing wild type EGFR incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    A-431 IC50
    0.685 μM
    Compound: AZD-9291
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    [PMID: 29534926]
    A-431 EC50
    0.7 μM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    [PMID: 28603991]
    A-431 IC50
    0.77 μM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    A-431 IC50
    0.77 μM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human A-431 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    A-431 IC50
    0.821 μM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A-431 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    A-431 IC50
    0.85 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    A-431 IC50
    0.893 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
    Antiproliferative activity against human A431 cells overexpressing wild-type EGFR after 72 hrs by SRB assay
    [PMID: 27131639]
    A-431 IC50
    0.945 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells harboring wild-type EGFR after 72 hrs by MTT assay
    [PMID: 30471829]
    A-431 EC50
    0.956 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    A-431 IC50
    0.956 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    [PMID: 28987609]
    A-431 IC50
    1.19 μM
    Compound: 4
    Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    A-431 IC50
    1.226 μM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 34218082]
    A-431 IC50
    1.24 μM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    A-431 IC50
    1.26 μM
    Compound: 5; AZD9291
    Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
    Antiproliferative activity against wild type EGFR expressing human A431 cells after 72 hrs by SRB assay
    [PMID: 29730192]
    A-431 IC50
    1.3 μM
    Compound: 4
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    A-431 IC50
    1.325 μM
    Compound: 4
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 36288657]
    A-431 IC50
    1.44 μM
    Compound: 4; AZD9291
    Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
    Antiproliferative activity human A431 cells incubated for 72 hrs by SRB assay
    [PMID: 31223440]
    A-431 IC50
    1.51 μM
    Compound: 6, AZD9291
    Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against human A431 cells overexpressing EGFR assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    A-431 IC50
    1.604 μM
    Compound: 3
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
    Antiproliferative activity against human A431 cells harboring wild type EGFR after 72 hrs by SRB assay
    [PMID: 28033579]
    A-431 IC50
    1310 nM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells expressing EGFR wildtype assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    A-431 IC50
    138.7 nM
    Compound: AZD9291
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    [PMID: 33459024]
    A-431 IC50
    2.035 nM
    Compound: 5
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A-431 cells harboring wild type EGFR assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    A-431 GI50
    40.1 nM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human A431 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    A-431 IC50
    5.32 μM
    Compound: Osimertinib
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A-431 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    A-431 IC50
    742 nM
    Compound: AZD9291
    Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human A431 cells expressing wild type EGFR assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    A-431 IC50
    795.2 nM
    Compound: AZD9291
    Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
    Cytotoxicity against human A-431 cells harboring wild-type EGFR measured after 72 hrs by celltiter-glo assay
    [PMID: 33667898]
    A-431 EC50
    830 nM
    Compound: 1
    Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against human A-431 cells expressing wild type EGFR assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    A-431 IC50
    84 nM
    Compound: Osimertinib
    Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    Antiproliferative activity against human A431 cells harboring EGFR wild type incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    A-431 CC50
    967 nM
    Compound: Osimertinib
    Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
    Cytotoxicity in human A431 cells assessed as reduction in cell viability incubated for 96 hrs by MTS method
    [PMID: 31560541]
    A549 IC50
    0.14 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human A549 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    A549 IC50
    0.31 μM
    Compound: 2
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    Cytotoxicity against human A549 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    [PMID: 30108918]
    A549 IC50
    0.335 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    A549 IC50
    0.445 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    A549 IC50
    0.462 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    A549 IC50
    0.53 μM
    Compound: osimertinib
    Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells harboring wild type EGFR assessed as reduction in cell viability after 72 hrs by MTT assay
    [PMID: 29853340]
    A549 IC50
    0.53 μM
    Compound: AZD
    Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring wild type EGFR after 72 hrs by MTT assay
    [PMID: 29466773]
    A549 IC50
    0.615 μM
    Compound: 6; AZD9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30530173]
    A549 IC50
    0.67 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    A549 IC50
    0.672 μM
    Compound: AZD9291
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human A549 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    A549 IC50
    0.72 μM
    Compound: 4
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    A549 IC50
    0.784 μM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human A549 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    A549 IC50
    0.87 μM
    Compound: AZD9291
    Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
    Cytotoxicity against human A549 cells expressing wild-type EGFR/K-ras mutant after 72 hrs by MTT assay
    [PMID: 29486953]
    A549 IC50
    0.9 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells harboring EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    A549 IC50
    1.557 nM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells expressing wild type EGFR assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    A549 EC50
    1.83 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human A549 cells harboring KRAS-G12S mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    A549 IC50
    1.87 μM
    Compound: 3
    Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 35696862]
    A549 IC50
    1.97 μM
    Compound: Osimertinib
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    A549 IC50
    150 nM
    Compound: 9; AZD9291
    Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
    Inhibition of EGF-stimulated wild type EGFR autophosphorylation expressed in human A549 cells by sandwich ELISA
    [PMID: 26756222]
    A549 IC50
    3.242 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 30471829]
    A549 GI50
    3.5 μM
    Compound: 5; AZD9291
    Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
    Inhibition of wild-type EGFR in human A549 cells assessed as growth inhibition after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    A549 IC50
    486 nM
    Compound: AZD9291
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    Antiproliferative activity against human A549 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    A549 IC50
    5 μM
    Compound: Osimertinib
    Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against wild type human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    ASPC1 IC50
    3.985 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
    Antiproliferative activity against human Aspc-1 cells after 72 hrs by MTT assay
    [PMID: 30471829]
    BaF3 IC50
    > 1 μM
    Compound: 65, AZD9291
    Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
    Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay
    [PMID: 26258521]
    BaF3 IC50
    > 3000 nM
    Compound: 4
    Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    Cytotoxicity against mouse BaF3 cells harboring EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by MTS assay
    [PMID: 34464874]
    BaF3 EC50
    > 5000 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Antiproliferative activity against mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    0.033 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M double mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36064123]
    BaF3 GI50
    0.347 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    BaF3 EC50
    0.545 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    Antiproliferative activity against mouse Ba/F3 cells harbouring Her2-A775_G776insYVMA mutant measured after 72 hrs by CellTiter-Glo assay
    [PMID: 35486541]
    BaF3 IC50
    0.859 μM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M/C797S triple mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 36064123]
    BaF3 IC50
    1 nM
    Compound: Osimertinib
    Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of EGFR del19 mutant in mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 GI50
    1.2 μM
    Compound: 5; AZD9291
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    Growth inhibition of mouse BAF3 cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    BaF3 IC50
    10.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    110 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    1100 nM
    Compound: Osimertinib
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 IC50
    1200 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR Ex19del/T790M/C797S mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    1320.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    14 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    1409.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    1475 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    1503.9 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M/C797S assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    154.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion GV mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    16 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing wild type EGFR incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 EC50
    16 nM
    Compound: Osimertinib
    Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR T790M exon19 deletion double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 EC50
    1748 nM
    Compound: Osimertinib
    Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EML4/ALK (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 EC50
    18 nM
    Compound: Osimertinib
    Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR exon19 deletion mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    2 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    2.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing L858R assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    2.885 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR 19Del/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 IC50
    2.893 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S triple mutant assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 EC50
    20 nM
    Compound: Osimertinib
    Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR T790M/L858R double mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    21.5 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR L858R/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    [PMID: 33459024]
    BaF3 EC50
    2956 nM
    Compound: 1
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R/C797S mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    BaF3 IC50
    3 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 EC50
    3.2 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R mutant after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    3.3 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    3.52 μM
    Compound: 5
    Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Cytotoxicity against mouse IL-3 dependent BaF3 cells assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    BaF3 IC50
    3.93 μM
    Compound: 4; AZD9291
    Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells transfected with EGFR L858R/T790M/C797S mutant (unknown origin) incubated for 72 hrs by resazurin dye based assay
    [PMID: 31223440]
    BaF3 IC50
    300.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion SVD mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    3100 nM
    Compound: Osimertinib
    Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
    Inhibition of phosphorylated EGFR del19/T790M/C797S triple mutant (unknown origin) expressed in mouse BaF3 cells incubated for 4 hrs by Alphascreen assay
    [PMID: 31689114]
    BaF3 EC50
    34 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
    Antiproliferative activity against mouse BAF3 cells harboring HER2 wild type after 72 hrs by resazurin dye-based fluorescence assay
    [PMID: 36518696]
    BaF3 IC50
    4 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR del19/T790M mutant incubated for 72 hrs by Cell Titer-Glo luminescent assay
    [PMID: 33459024]
    BaF3 IC50
    4.27 μM
    Compound: 5
    Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against mouse BaF3 cells stably expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    BaF3 IC50
    4.3 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Del19 assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    4.427 μM
    Compound: AZD9291; 5
    Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    BaF3 IC50
    4.5 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing De119/T790M assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 IC50
    4.61 μM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    BaF3 IC50
    5.11 μM
    Compound: 4; AZD9291
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
    Cytotoxicity against mouse BAF3 cells incubated for 72 hrs by resazurin dye based assay
    [PMID: 31223440]
    BaF3 IC50
    5.15 μM
    Compound: AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR L858R/T790M/C797S mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    BaF3 IC50
    5.47 μM
    Compound: 6, AZD9291
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against mouse BAF3 cells harboring EGFR 19D/T790M/C797S mutant assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    BaF3 IC50
    53.1 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR WT assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    6 nM
    Compound: 1
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    Cytotoxicity against mouse BaF3 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 96 hrs by CellTiter-Glo assay
    [PMID: 37197473]
    BaF3 EC50
    6 nM
    Compound: Osimertinib
    Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of EGFR L858R mutant (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    6.071 nM
    Compound: 5
    Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against mouse BaF3 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 35446588]
    BaF3 IC50
    60.6 nM
    Compound: Osimertinib
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing Ex20 insertion NPG mutant assessed as cell viability measured after 72 hrs hrs by CellTiter Glo assay
    [PMID: 36384036]
    BaF3 EC50
    66 nM
    Compound: Osimertinib
    Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    Inhibition of wild type EGFR (unknown origin) transfected in mouse BAF3 cells assessed as reduction in cell viability after 72 hrs by MTS assay
    [PMID: 28528303]
    BaF3 IC50
    780 nM
    Compound: Osimertinib
    Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of EGFR del19/T790M/C797S triple mutant in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BaF3 IC50
    8 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M mutant incubated for 72 hrs in absence of cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    800 nM
    Compound: AZD9291
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    Antiproliferative activity against mouse BaF3 cells expressing EGFR L858R/T790M/C797S mutant incubated for 72 hrs in presence of 1 ug/ml cetuximab by Cell Titer-Glo assay
    [PMID: 34668706]
    BaF3 IC50
    81 nM
    Compound: Osimertinib
    Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    Inhibition of wild type EGFR in mouse BAF3 cells assessed as reduction in cell proliferation incubated for 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    BEAS-2B IC50
    14.9 μM
    Compound: 1; AZD9291
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
    Antiproliferative activity against human BEAS2B cells after 72 hrs by MTS assay
    [PMID: 28716641]
    BJ IC50
    > 10 μM
    Compound: AZD9291
    Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human BJ cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    Calu-3 IC50
    0.75 μM
    Compound: Osimertinib
    Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human Calu3 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    Calu-3 GI50
    264 nM
    Compound: 8
    Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human Calu3 cells assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    Calu-6 IC50
    5.86 μM
    Compound: Osimertinib
    Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
    Antiproliferative activity against human Calu6 cells harboring WT EGFR after 72 hrs by MTS assay
    [PMID: 30442506]
    CHO GI50
    4.2 μM
    Compound: 5; AZD9291
    Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
    Growth inhibition of CHO cells after 72 hrs by CellTiter-Glo assay
    [PMID: 28282122]
    CL97 IC50
    0.1 μM
    Compound: Osimertinib
    Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human CL97 cells harbouring EGFR G719A/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    EA.hy 926 IC50
    1.161 μM
    Compound: Osimertinib
    Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Cytotoxicity against human EA.hy 926 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    HaCaT IC50
    73.7 nM
    Compound: 5; AZD9291
    Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
    Inhibition of wild type EGFR phosphorylation in human HaCaT cells incubated for 3 hrs by ELISA method
    [PMID: 27433829]
    HCC827 EC50
    < 0.014 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human HCC827 cells harboring EGFR-delE746_A750 mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    HCC827 IC50
    0.00173 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human HCC827 cells expressing EGFR del119 mutant assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    HCC827 IC50
    0.00248 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-HCC827 cells expressing EGFR del19 incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    HCC827 IC50
    0.003 μM
    Compound: 4
    Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    HCC827 IC50
    0.011 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
    Antiproliferative activity against human HCC827 cells harboring EGFR mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    HCC827 IC50
    0.027 μM
    Compound: osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFR E746 to A750 deletion mutant after 72 hrs by MTT assay
    [PMID: 29853340]
    HCC827 IC50
    0.027 μM
    Compound: AZD
    Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFR E746-A750 deletion mutant after 72 hrs by MTT assay
    [PMID: 29466773]
    HCC827 IC50
    0.036 μM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells harboring EGFRDel19 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    HCC827 IC50
    0.2 μM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human HCC827 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    HCC827 IC50
    0.97 nM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells expressing EGFR del19 mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    HCC827 IC50
    1 nM
    Compound: Osimertinib
    Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells expressing EGFR deletion19 mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    HCC827 IC50
    25.4 nM
    Compound: AZD9291
    Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCC827 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    HEK293 IC50
    0.57 μM
    Compound: AZD9291
    Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
    Inhibition of human ERG expressed in HEK293 cells by lonWorks Quattro analysis
    [PMID: 28426996]
    HEK293-A IC50
    2.418 μM
    Compound: AZD9291
    Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human HEK293A cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    HeLa IC50
    0.975 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    HeLa IC50
    1.83 μM
    Compound: AZD9291
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    HepG2 IC50
    1.605 μM
    Compound: 6; AZD9291
    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: 30530173]
    HK-2 IC50
    2.399 μM
    Compound: Osimertinib
    Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Cytotoxicity against human HK-2 cells assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    HK-2 IC50
    2.719 μM
    Compound: AZD9291
    Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against HK-2 cells assessed as reduction in cell viability by MTT assay
    [PMID: 33429247]
    HK-2 IC50
    3.565 μM
    Compound: AZD9291
    Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human HK2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    HT-29 IC50
    0.65 μM
    Compound: AZD9291
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay
    [PMID: 29486953]
    HUVEC IC50
    7.278 μM
    Compound: AZD9291
    Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
    Cytotoxicity against HUVEC assessed as reduction in cell viability measured after 72 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 32619886]
    KG-1 IC50
    0.53 μM
    Compound: Osimertinib
    Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human KG-1 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    L02 IC50
    > 40 μM
    Compound: Osimertinib
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    L02 IC50
    > 50 μM
    Compound: AZD9291
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Cytotoxicity against human L02 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    L02 IC50
    0.3 μM
    Compound: AZD9291
    Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
    Cytotoxicity against human HL7702 cells measured after 72 hrs by sulforhodamine B assay
    [PMID: 31889606]
    L02 IC50
    1.602 μM
    Compound: AZD9291
    Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Cytotoxicity against human LO2 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    L02 IC50
    1.975 μM
    Compound: AZD9291
    Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
    Cytotoxicity against human L02 cells assessed as reduction in cell viability by MTT assay
    [PMID: 33429247]
    LoVo IC50
    480 nM
    Compound: AZD9291
    Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
    Inhibition of wild type EGFR phosphorylation in human LoVo cells preincubated for 2 hrs followed by EGF stimulation measured after 30 mins by ELISA
    [PMID: 26968253]
    LoVo IC50
    480 μM
    Compound: 8
    Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
    Inhibition of wild type EGFR phosphorylation in human LoVo cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    MCF7 IC50
    3.67 μM
    Compound: AZD9291
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay
    [PMID: 32679450]
    MDA-MB-468 IC50
    1.3 μM
    Compound: Osimertinib
    Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-468 cells incubated for 72 hrs by MTT assay
    [PMID: 32961382]
    NCI-H1299 IC50
    > 10 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1299 cells assessed as inhibition of cell proliferation measured after 72 hrs by SRB assay
    [PMID: 35178175]
    NCI-H1299 IC50
    2.84 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR assessed as inhibition in cell viability after 72 hrs by CCK8 assay
    [PMID: 34794818]
    NCI-H1299 IC50
    3.24 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1299 cells expressing wild type EGFR incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    NCI-H1975 EC50
    < 0.014 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR-L858R/T790M double mutant incubated for 96 hrs measured on day 5 by CellTiterGlo assay
    [PMID: 28853575]
    NCI-H1975 IC50
    < 1 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    NCI-H1975 IC50
    0.011 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant by MTT assay
    [PMID: 33429247]
    NCI-H1975 IC50
    0.012 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTT assay
    [PMID: 31787359]
    NCI-H1975 IC50
    0.013 μM
    Compound: 2
    Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    Cytotoxicity against human NCI-H1975 cells assessed as cell growth inhibition after 4 days by CCK-8 assay
    [PMID: 30108918]
    NCI-H1975 IC50
    0.014 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    NCI-H1975 IC50
    0.0148 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant assessed as inhibition in cell viability after 72 hrs by CCK-8 assay
    [PMID: 34794818]
    NCI-H1975 IC50
    0.016 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability measured after 72 hrs by WST assay
    [PMID: 32550993]
    NCI-H1975 IC50
    0.019 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/ L858R double mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    NCI-H1975 EC50
    0.019 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as growth inhibition after 96 hrs by CellTiter-Glo assay
    [PMID: 28603991]
    NCI-H1975 IC50
    0.019 μM
    Compound: osimertinib
    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: 29853340]
    NCI-H1975 IC50
    0.019 μM
    Compound: AZD
    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: 29466773]
    NCI-H1975 IC50
    0.023 μM
    Compound: AZD-9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by MTT assay
    [PMID: 29534926]
    NCI-H1975 IC50
    0.03 μM
    Compound: 4; AZD9291
    Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
    Antiproliferative activity human NCI-H1975 cells incubated for 72 hrs by SRB assay
    [PMID: 31223440]
    NCI-H1975 IC50
    0.03 μM
    Compound: 3
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by SRB assay
    [PMID: 28033579]
    NCI-H1975 IC50
    0.0305 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M incubated for 72 hrs by CCK-8 assay
    [PMID: 35691176]
    NCI-H1975 IC50
    0.041 μM
    Compound: 5; AZD9291
    Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
    Antiproliferative activity against EGFR T790M/L858R double mutant expressing human NCI-H1975 cells after 72 hrs by SRB assay
    [PMID: 29730192]
    NCI-H1975 IC50
    0.044 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31951960]
    NCI-H1975 IC50
    0.05 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M double mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    NCI-H1975 IC50
    0.052 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR T790M/L858R mutant after 72 hrs by SRB assay
    [PMID: 27131639]
    NCI-H1975 IC50
    0.06 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    NCI-H1975 IC50
    0.06 μM
    Compound: AZD9291
    Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    Cytotoxicity against human NCI-H1975 cells expressing EGFR L858R/T790M double mutant after 72 hrs by MTT assay
    [PMID: 29486953]
    NCI-H1975 IC50
    0.064 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant assessed as inhibition of cell proliferation incubated for 72 hrs by sulforhodamine B colorimetric assay
    [PMID: 28987609]
    NCI-H1975 IC50
    0.07 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells incubated for 72 hrs by MTS assay
    [PMID: 31718182]
    NCI-H1975 IC50
    0.072 μM
    Compound: 3
    Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
    Antiproliferative activity against human H1975 cells assessed as cell viability after 72 hrs by MTT assay
    [PMID: 35696862]
    NCI-H1975 IC50
    0.073 μM
    Compound: 3; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell growth after 72 hrs by MTT assay
    [PMID: 31683104]
    NCI-H1975 IC50
    0.073 μM
    Compound: 6; AZD9291
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 30530173]
    NCI-H1975 IC50
    0.076 μM
    Compound: AZD9291
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability measured by MTT assay
    [PMID: 34534838]
    NCI-H1975 IC50
    0.091 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability incubated for 72 hrs by CCK8 assay
    [PMID: 34218082]
    NCI-H1975 IC50
    0.095 μM
    Compound: 4
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R mutant assessed as reduction in cell growth incubated for 72 hrs by MTT assay
    [PMID: 36288657]
    NCI-H1975 IC50
    0.096 μM
    Compound: 6; AZD-9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTT assay
    [PMID: 30471829]
    NCI-H1975 IC50
    0.1 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M mutant assessed as reduction in cell viability measured after 72 hrs by CCK8 assay
    [PMID: 35178185]
    NCI-H1975 IC50
    0.1 μM
    Compound: 4
    Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
    Growth inhibition of human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 30472599]
    NCI-H1975 IC50
    0.125 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    0.13 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant after 72 hrs by resazurin dye based assay
    [PMID: 30429956]
    NCI-H1975 IC50
    0.74 μM
    Compound: 6, AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M mutant assessed as reduction in cell viability by CCK8 assay
    [PMID: 32631532]
    NCI-H1975 IC50
    0.98 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 33640672]
    NCI-H1975 IC50
    10.5 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant after 72 hrs by MTS assay
    [PMID: 28716641]
    NCI-H1975 IC50
    15 nM
    Compound: 9; AZD9291
    Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
    Inhibition of EGFR L858R/T790M double mutant autophosphorylation in human NCI-H1975 cells after 2 hrs by sandwich ELISA
    [PMID: 26756222]
    NCI-H1975 IC50
    15 μM
    Compound: 8
    Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
    Inhibition of EGFR L858R/T970M double mutant phosphorylation in human NCI-H1975 cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    NCI-H1975 IC50
    17 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells expressing EGFR L858R/T790M mutant assessed as inhibition of cell proliferation incubated for 72 hrs by MTT assay
    [PMID: 35254067]
    NCI-H1975 IC50
    18.21 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR L858R/T790M double mutant measured after 72 hrs by celltiter-glo assay
    [PMID: 33667898]
    NCI-H1975 IC50
    2.08 μM
    Compound: Osimertinib
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
    Cytotoxicity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs under hypoxic condition by MTT assay
    [PMID: 33640672]
    NCI-H1975 GI50
    2.8 nM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    NCI-H1975 GI50
    24 nM
    Compound: 8
    Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human NCI-H1975 cells harboring EGFR L858R/T970M double mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    NCI-H1975 IC50
    3.1 μM
    Compound: Osimertinib
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H1975 cells harbouring EGFR L858R/T790M/C797S mutant incubated for 72 hrs by MTS assay
    [PMID: 31718182]
    NCI-H1975 IC50
    3.85 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells harbouring wild type Akt3 assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    4.32 μM
    Compound: 1
    Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human NCI-H1975 cells harbouring Akt3 T305A/S472A mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 36173763]
    NCI-H1975 IC50
    42 nM
    Compound: AZD9291
    Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    Antiproliferative activity against human H1975 cells expressing EGFR L858R/T790M mutant assessed as cell growth inhibition measured after 72 hrs by MTT assay
    [PMID: 32883633]
    NCI-H1975 IC50
    47.2 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells after 72 hrs by MTT assay
    [PMID: 29576272]
    NCI-H1975 IC50
    47.3 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by sulforhodamine B assay
    [PMID: 33459024]
    NCI-H1975 IC50
    73.4 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H1975 cells harboring EGFR T790M/L858R double mutant assessed as inhibition of cell viability measured after 72 hrs by MTT assay
    [PMID: 32679450]
    NCI-H292 IC50
    0.22 μM
    Compound: 1
    Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
    Antiproliferative activity against human NCI-H292 cells expressing wild type EGFR assessed as reduction in cell viability measured after 72 hrs by WST assay
    [PMID: 32550993]
    NCI-H292 IC50
    0.924 nM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
    Antiproliferative activity against human NCI-H292 cells harboring wild-type EGFR by MTT assay
    [PMID: 33429247]
    NCI-H292 IC50
    1.084 μM
    Compound: AZD9291
    Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human NCI-H292 cells expressing EGFR assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    NCI-H460 IC50
    415.9 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
    Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTS assay
    [PMID: 28716641]
    PC-9 IC50
    < 0.01 μM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human PC9 cells harbouring EGFR delE746-A750 mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31446247]
    PC-9 IC50
    > 1000 nM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    Antiproliferative activity against human PC9 cells harboring EGFR del19/T790M/C797S triple mutant incubated for 96 hrs by Celltiter-Glo luminescent cell viability assay
    [PMID: 31689114]
    PC-9 IC50
    0.011 nM
    Compound: AZD9291
    Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
    Antiproliferative activity against human PC-9 cells harboring EGFR L858R mutant by MTT assay
    [PMID: 33429247]
    PC-9 IC50
    0.011 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human PC-9 cells assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    PC-9 IC50
    0.016 μM
    Compound: AZD9291
    Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    Antiproliferative activity against human PC9 cells expressing EGFR L858R mutant assessed as reduction in cell viability incubated for 72 hrs by MTT assay
    [PMID: 31581004]
    PC-9 IC50
    0.023 nM
    Compound: Osimertinib
    Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    Antiproliferative activity against human PC-9 cells expressing EGFR Del19 mutant assessed as inhibition of cell growth measured after 48 to 72 hrs by MTT assay
    [PMID: 37087886]
    PC-9 IC50
    0.16 μM
    Compound: Osimertinib
    Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
    Antiproliferative activity against human PC9 cells harboring EGFR mutant after 72 hrs by MTS assay
    [PMID: 30442506]
    PC-9 IC50
    17 nM
    Compound: AZD9291
    Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
    Inhibition of EGFR Del ex19 mutant phosphorylation in human PC9 cells preincubated for 2 hrs by ELISA
    [PMID: 26968253]
    PC-9 IC50
    17 μM
    Compound: 8
    Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
    Inhibition of EGFR exon 19 deletion activating mutant phosphorylation in human PC9 cells after 2 hrs by fluorescence assay
    [PMID: 25271963]
    PC-9 GI50
    23 nM
    Compound: 8
    Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    Cytotoxicity against human PC9 cells harboring EGFR exon 19 deletion activating mutant assessed as growth inhibition after 72 hrs by SYTOX green nucleic acid staining-based fluorescence assay
    [PMID: 25271963]
    PC-9 IC50
    3.21 μM
    Compound: AZD9291; 5
    Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    Antiproliferative activity against human PC-9 cells expressing EGFR 19Del/T790M/C797S triple mutation assessed as inhibition of cell proliferation measured after 72 hrs by CCK8 assay
    [PMID: 35178175]
    PC-9 IC50
    3.248 μM
    Compound: AZD9291
    Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human PC-9 cells expressing EGFR L858R/T790M/C797S mutant assessed as inhibition of cell growth incubated for 72 hrs by CCK-8 assay
    [PMID: 35447433]
    PC-9 IC50
    5.431 nM
    Compound: 5
    Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    Antiproliferative activity against human osimertinib-resistant PC-9 cells harboring EGFR 19 del/T790M/C797S mutant assessed as reduction in cell viability incubated for 72 hrs by CCK-8 assay
    [PMID: 35446588]
    PC-9 IC50
    56 nM
    Compound: 9; AZD9291
    Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
    Inhibition of EGFR deletion mutant autophosphorylation in human PC9 cells after 2 hrs by sandwich ELISA
    [PMID: 26756222]
    PC-9 IC50
    6.5 nM
    Compound: 1; AZD9291
    Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
    Antiproliferative activity against human PC9 cells harboring EGFR exon 19 deletion mutant after 72 hrs by MTS assay
    [PMID: 28716641]
    Sf9 IC50
    0.002 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M double mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo k
    [PMID: 31718182]
    Sf9 IC50
    0.09 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR L858R/T790M/C797S mutant (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo ki
    [PMID: 31718182]
    Sf9 IC50
    1.23 μM
    Compound: Osimertinib
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
    Inhibition of C-terminal His-tagged/ N-terminal GST-tagged recombinant human EGFR (668 to 1210 residues) expressed in a Baculovirus infected Sf9 cell expression system using poly-EY as substrate incubated for 30 mins by ADP-Glo kinase assay
    [PMID: 31718182]
    Sf9 IC50
    20.8 nM
    Compound: 6; AZD-9291
    Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    Inhibition of human N-terminal GST-tagged EGFR T790M/L858R double mutant (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    [PMID: 30471829]
    Sf9 IC50
    567.5 nM
    Compound: 6; AZD-9291
    Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    Inhibition of wild-type human N-terminal GST-tagged EGFR (695 to end residues) expressed in baculovirus infected Sf9 insect cells using Poly (4:1 Glu, Tyr) as substrate after 60 mins in presence of ATP by ADP-Glo assay
    [PMID: 30471829]
    U-87MG ATCC IC50
    4.5 μM
    Compound: 4
    Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    Antiproliferative activity against human U-87MG cells harboring wild type EGFR assessed as inhibition of cell growth by MTT assay
    [PMID: 31869655]
    Vero CC50
    13.23 μM
    Compound: Osimertinib
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    Cell viability measured by CellTiter-Glo assay in Vero cells at MOI 0.05 after 72hr
    10.1101/2020.03.20.999730
    Vero IC50
    3.26 μM
    Compound: Osimertinib
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    Antiviral activity against SARS-CoV-2 (viral titer) measured by plaque assay in Vero cells at MOI 0.0125 after 24 hr
    10.1101/2020.03.20.999730
    体外研究
    (In Vitro)

    Osimertinib (AZD9291) (0-10 μM;72 小时) 显著抑制细胞增殖,IC50 分别为 41、26、41 和 31 nM[2]
    Osimertinib (0-10 μM;72 小时) 抑制细胞增殖 (携带 T790M 突变、外显子 19del+T790M 或 L858R+T790M 的 Ba/F3 细胞),IC50 分别为 6、7 和 74 nM[2]
    Osimertinib 在两种 EGFR 细胞系:致敏突变体 (PC-9 的平均 IC50 为 8 nM) 和 T790M (H1975 和 PC-9VanR 的平均 IC50 为 11 和 40 nM) 中具有高表型效力[2]
    Osimertinib (0-10 μM;72 小时) 抑制携带 EGFR 外显子 20 插入突变的 Ba/F3 细胞,对于 A763_Y764insFQEA (FQEA)、Y764_V765insHH (HH)、A767_V769dupASV (ASV) 和 D770_N771insNPG (NPG) 细胞的 IC50 范围为 16 到 701 nM[2]

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

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring a T790M mutation, exon 19del+T790M, or L858R+T790M)
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=6, 7, 74 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: PC-9, H3255, PC-9ER, and H1975 cells
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Dramatically inhibited cell proliferation (IC50s=41, 26, 41, 31 nM, respectively)

    Cell Proliferation Assay[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 20 insertion mutations: FQEA, HH, ASV, NPG )
    Concentration: 0.0001, 0.001, 0.01, 0.1, 1, 10 μM
    Incubation Time: 72 hours
    Result: Inhibited cell proliferation (IC50s=16, 701, 230, 38 nM, respectively)

    Apoptosis Analysis[2]

    Cell Line: Ba/F3 cells (harboring EGFR exon 19del+T790M or EGFR L858R+T790M)
    Concentration: 0.1 μM
    Incubation Time: 48 hours
    Result: Induced apoptosis with the rates of 40.9% and 90% in EGFR T790M positive mutations cells, respectively.
    体内研究
    (In Vivo)

    Osimertinib (0.1-25 mg/kg;口服每日一次,持续 14 天) 在 PC-9 (ex19del) 和 H1975 (L858R/T790M) 肿瘤异种移植模型中诱导显著的剂量依赖性消退[1]

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

    Animal Model: PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models[1]
    Dosage: 0.1-10 mg/kg (PC-9 xenograft models); 0.5- 25 mg/kg (H1975 xenograft models)
    Administration: p.o.; daily for 14 days
    Result: Induced significant dose-dependent regression in both PC-9 (ex19del) and H1975 (L858R/T790M) tumor xenograft models.
    Clinical Trial
    分子量

    499.61

    Formula

    C28H33N7O2

    CAS 号
    性状

    固体

    颜色

    Light yellow to brown

    中文名称

    奥斯替尼;奥希替尼

    运输条件

    Room temperature in continental US; may vary elsewhere.

    储存方式
    Powder -20°C 3 years
    4°C 2 years
    In solvent -80°C 2 years
    -20°C 1 year
    溶解性数据
    细胞实验: 

    DMSO 中的溶解度 : 100 mg/mL (200.16 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 2.0016 mL 10.0078 mL 20.0156 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    • 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    90% Corn Oil

      Solubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液

      此方案可获得 ≥ 2.5 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 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。

    • 方案 二

      请依序添加每种溶剂: 5% DMSO    40% PEG300    5% Tween-80    50% Saline

      Solubility: ≥ 2.5 mg/mL (5.00 mM); 澄清溶液

    以下溶解方案,请直接配制工作液。建议现用现配,在短期内尽快用完。 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: 0.5% HPMC/1% Tween-80 in Saline water

      Solubility: 5 mg/mL (10.01 mM); Suspened solution; 超声助溶 (<60°C)

    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)。
    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: 99.96%

    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, 2 years; -20°C, 1 year。-80°C储存时,请在2年内使用, -20°C储存时,请在1年内使用。

    可选溶剂 浓度 溶剂体积 质量 1 mg 5 mg 10 mg 25 mg
    DMSO 1 mM 2.0016 mL 10.0078 mL 20.0156 mL 50.0390 mL
    5 mM 0.4003 mL 2.0016 mL 4.0031 mL 10.0078 mL
    10 mM 0.2002 mL 1.0008 mL 2.0016 mL 5.0039 mL
    15 mM 0.1334 mL 0.6672 mL 1.3344 mL 3.3359 mL
    20 mM 0.1001 mL 0.5004 mL 1.0008 mL 2.5020 mL
    25 mM 0.0801 mL 0.4003 mL 0.8006 mL 2.0016 mL
    30 mM 0.0667 mL 0.3336 mL 0.6672 mL 1.6680 mL
    40 mM 0.0500 mL 0.2502 mL 0.5004 mL 1.2510 mL
    50 mM 0.0400 mL 0.2002 mL 0.4003 mL 1.0008 mL
    60 mM 0.0334 mL 0.1668 mL 0.3336 mL 0.8340 mL
    80 mM 0.0250 mL 0.1251 mL 0.2502 mL 0.6255 mL
    100 mM 0.0200 mL 0.1001 mL 0.2002 mL 0.5004 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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