1. PI3K/Akt/mTOR Apoptosis
  2. PI3K Apoptosis
  3. Buparlisib

Buparlisib  (Synonyms: 布帕尼西; BKM120; NVP-BKM120)

目录号: HY-70063 纯度: 99.82%
Data Sheet SDS COA 产品使用指南 技术支持

Buparlisib (BKM120; NVP-BKM120) 是一种 pan-class I PI3K 抑制剂,作用于 p110α/p110β/p110δ/p110γIC50 分别为 52 nM/166 nM/116 nM/262 nM。

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Buparlisib Chemical Structure

Buparlisib Chemical Structure

CAS No. : 944396-07-0

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Customer Review

Other Forms of Buparlisib:

MCE 顾客使用本产品发表的 72 篇科研文献

WB

    Buparlisib purchased from MCE. Usage Cited in: Cancer Lett. 2019 Jan;440-441:54-63.  [Abstract]

    The cells are transfected with either the negative control (siNC) or BTF3 siRNA for 12 hours followed by BKM-120 or AZD-6482 treatment for 48 hours. The protein abundance is determined by an immunoblotting analysis.

    Buparlisib purchased from MCE. Usage Cited in: Brain Behav. 2018 Nov;8(11):e01123.  [Abstract]

    The effect of BKM120 on AKT phosphorylation is examined by Western blot.

    Buparlisib purchased from MCE. Usage Cited in: PLoS One. 2018 Jul 5;13(7):e0200014.  [Abstract]

    Representative immunoblots of control and NHARAS treated with Buparlisib for 24 h.

    Buparlisib purchased from MCE. Usage Cited in: Prostate. 2018 Feb;78(3):166-177.  [Abstract]

    Western blot analysis of p-AKT (Ser473) in stable cell lines (Vector-DU145 and GOLM1-DU145) treated with 200 nM, 500 nM or 1 μM BKM120.

    Buparlisib purchased from MCE. Usage Cited in: Nat Med. 2016 Jul;22(7):723-6.  [Abstract]

    Selective response of HER2-positive PDX DF-BM355 to the combination of BKM120/RAD001. Western blot analysis of lysates from vehicle-treated or BKM120-treated DF-BM355 in vivo.

    Buparlisib purchased from MCE. Usage Cited in: Oncogene. 2016 Jul 7;35(27):3607-12.  [Abstract]

    (A) Immunoblot analyses in HCC1569 cells treated with BYL719, KIN193 (MedChemexpress) or BKM120 (μM). (B, C) Immunoblot analyses in BT474 and BT474-shPTEN cells treated as indicated in (A).
    • 生物活性

    • 实验参考方法

    • 纯度 & 产品资料

    • 参考文献

    生物活性

    Buparlisib (BKM120; NVP-BKM120) is a pan-class I PI3K inhibitor, with IC50s of 52, 166, 116 and 262 nM for p110α, p110β, p110δ and p110γ, respectively.

    IC50 & Target[1]

    p110α

    52 nM (IC50)

    p110α-H1047R

    58 nM (IC50)

    p110α-E545K

    99 nM (IC50)

    p110δ

    116 nM (IC50)

    p110β

    166 nM (IC50)

    p110γ

    262 nM (IC50)

    Vps34

    2.4 μM (IC50)

    mTOR

    4.6 μM (IC50)

    细胞效力
    (Cellular Effect)
    Cell Line Type Value Description References
    A2780 EC50
    0.055 μM
    Compound: 15, NVP-BKM120
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human A2780 cells after 1 hr
    [PMID: 24900266]
    A2780 EC50
    0.074 μM
    Compound: 15, NVP-BKM120
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human A2780 cells after 1 hr
    [PMID: 24900266]
    A2780 EC50
    0.52 μM
    Compound: 15, NVP-BKM120
    Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay
    Antiproliferative activity against human A2780 cells after 3 days by CellTiter-Glo assay
    [PMID: 24900266]
    A2780 GI50
    0.635 nM
    Compound: 15, NVP-BKM120
    Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay
    Cytotoxicity against PTEN-deficient human A2780 cells after 3 days by CellTiterGlo assay
    [PMID: 24900266]
    A-431 IC50
    1.03 μM
    Compound: 5a
    Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human A431 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    A549 IC50
    1.51 μM
    Compound: 5a
    Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human A549 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    A549 IC50
    2.07 μM
    Compound: BKM120
    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: 25765909]
    Bel-7402 IC50
    1.92 μM
    Compound: 5a
    Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human Bel7402 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    Bel-7402 IC50
    13 μM
    Compound: 4; BKM120
    Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
    Antiproliferative activity against human Bel7402 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    BGC-823 IC50
    1.43 μM
    Compound: 5a
    Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human BGC823 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    Capan-2 IC50
    42 μM
    Compound: 4; BKM120
    Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
    Antiproliferative activity against human Capan2 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    D283 Med IC50
    0.279 μM
    Compound: BKM120
    Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay
    Cytotoxicity against human D283 Med cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay
    [PMID: 33636537]
    Daoy IC50
    0.279 μM
    Compound: BKM120
    Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay
    Cytotoxicity against human Daoy cells assessed as reduction in cell viability incubated for 48 hrs by Cell TiterGlo luminescent assay
    [PMID: 33636537]
    DU-145 EC50
    0.073 μM
    Compound: 15, NVP-BKM120
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in human DU145 cells harboring LKB1 mutation after 1 hr
    [PMID: 24900266]
    DU-145 IC50
    0.91 μM
    Compound: 5a
    Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human DU145 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    DU-145 IC50
    45 μM
    Compound: 4; BKM120
    Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
    Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HCT-116 IC50
    0.48 μM
    Compound: BKM120
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 72 hrs by MTT assay
    [PMID: 25765909]
    HCT-116 IC50
    1.3 μM
    Compound: 4; BKM120
    Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HCT116 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HCT-8 IC50
    1.7 μM
    Compound: 4; BKM120
    Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HCT8 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HeLa IC50
    1.17 μM
    Compound: 5a
    Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human HeLa cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    HeLa IC50
    4.34 μM
    Compound: BKM120
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    Antiproliferative activity against human HeLa cells after 72 hrs by MTT assay
    [PMID: 25765909]
    HepG2 IC50
    3.2 μM
    Compound: 4; BKM120
    Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HGC-27 IC50
    0.99 μM
    Compound: 4; BKM120
    Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HGC27 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HL-60 IC50
    1.51 μM
    Compound: BKM120
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human HL-60 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    [PMID: 36272186]
    HT-1080 IC50
    2.08 μM
    Compound: 5a
    Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human HT1080 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    Huh-7 IC50
    1.51 μM
    Compound: 5a
    Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human HuH7 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    Huh-7 IC50
    2 μM
    Compound: 4; BKM120
    Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
    Antiproliferative activity against human HuH7 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    HUVEC IC50
    0.886 μM
    Compound: NVP-BKM120; BKM
    Cytotoxicity against HUVEC after 72 hrs by MTT assay
    Cytotoxicity against HUVEC after 72 hrs by MTT assay
    [PMID: 30034607]
    K562 IC50
    0.73 μM
    Compound: BKM120
    Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    [PMID: 36272186]
    K562 IC50
    1.1 μM
    Compound: 5a
    Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human K562 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    K562 IC50
    7.9 μM
    Compound: 4; BKM120
    Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
    Antiproliferative activity against human K562 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MCF7 EC50
    < 0.1 μM
    Compound: 15, NVP-BKM120
    Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr
    Inhibition of PI3Kalpha E545K mutant-mediated AKT Ser473 phosphorylation in human MCF7 cells after 1 hr
    [PMID: 24900266]
    MCF7 IC50
    0.206 μM
    Compound: NVP-BKM120; BKM
    Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells harboring PIK3CA E545K mutant after 72 hrs by MTT assay
    [PMID: 30034607]
    MCF7 IC50
    1 μM
    Compound: BKM120
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 25765909]
    MCF7 IC50
    1.5 μM
    Compound: 5a
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MCF7 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    MCF7 IC50
    11.05 μM
    Compound: Buparlisib
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    MCF7 IC50
    5.7 μM
    Compound: 4; BKM120
    Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
    Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MDA-MB-231 IC50
    1.88 μM
    Compound: Buparlisib
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    MDA-MB-453 IC50
    0.37 μM
    Compound: 4; BKM120
    Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
    Antiproliferative activity against human MDA-MB-453 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    MDA-MB-468 IC50
    3.97 μM
    Compound: BKM120
    Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay
    Antiproliferative activity against human MDA-MB-468 cells measured after 7 days by Celltiter-glo assay
    [PMID: 33309164]
    MOLT-4 IC50
    0.8 μM
    Compound: 5a
    Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human MOLT4 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    MV4-11 IC50
    0.73 μM
    Compound: BKM120
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    Antiproliferative activity against human MV4-11 cells assessed as inhibition of cell proliferation incubated for 72 hrs by CCK8 assay
    [PMID: 36272186]
    NCI-H1299 IC50
    3.6 μM
    Compound: 4; BKM120
    Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
    Antiproliferative activity against human NCI-H1299 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    NCI-H460 IC50
    3.2 μM
    Compound: 4; BKM120
    Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
    Antiproliferative activity against human NCI-H460 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    NCI-N87 IC50
    0.66 μM
    Compound: 5a
    Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human NCI-N87 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    PANC-1 IC50
    1.83 μM
    Compound: 5a
    Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human PANC1 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    PC-3 IC50
    5.34 μM
    Compound: Buparlisib
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    Cytotoxicity against human PC3 cells after 72 hrs by MTT assay
    [PMID: 29107429]
    SGC-7901 IC50
    1.24 μM
    Compound: 5a
    Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human SGC7901 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    SW1990 IC50
    1.3 μM
    Compound: 4; BKM120
    Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
    Antiproliferative activity against human SW1990 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    T47D IC50
    0.286 μM
    Compound: NVP-BKM120; BKM
    Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay
    Antiproliferative activity against human T47D cells harboring PI3KCA H1047R mutant after 72 hrs by MTT assay
    [PMID: 30034607]
    T47D IC50
    6.92 μM
    Compound: Buparlisib
    Cytotoxicity against human T47D cells after 72 hrs by MTT assay
    Cytotoxicity against human T47D cells after 72 hrs by MTT assay
    [PMID: 29107429]
    THP-1 IC50
    12 μM
    Compound: 4; BKM120
    Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay
    Antiproliferative activity against human THP1 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    U-87MG ATCC EC50
    0.13 μM
    Compound: 15, NVP-BKM120
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr
    Inhibition of PI3K-mediated AKT Ser473 phosphorylation in PTEN-deficient human U87MG cells after 1 hr
    [PMID: 24900266]
    U-87MG ATCC IC50
    1.64 μM
    Compound: BKM120
    Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay
    Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay
    [PMID: 25765909]
    U-87MG ATCC IC50
    4.8 μM
    Compound: 4; BKM120
    Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
    Antiproliferative activity against human U87 cells after 96 hrs by MTT assay
    [PMID: 31117517]
    U-937 IC50
    0.58 μM
    Compound: 5a
    Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay
    Antiproliferative activity against human U937 cells after 72 hrs by CCK8 assay
    [PMID: 27427973]
    体外研究
    (In Vitro)

    Buparlisib (NVP-BKM120) 对 I 类 PI3K(包括最常见的 p110α 突变体)表现出 50-300 nM 的活性。此外,NVP-BKM120 对 III 类和 IV 类 PI3K 表现出较低的效力,其中分别观察到 2、5、>5 和 >25 μM 的生化活性,用于抑制 VPS34、mTOR、DNAPK 和 PI4K[1]。Buparlisib (NVP-BKM120) 以剂量和时间依赖性方式诱导多发性骨髓瘤 (MM) 细胞凋亡。浓度≥10 μM 的 Buparlisib (NVP-BKM120) 在 24 小时后在所有测试的 MM 细胞系中诱导显着细胞凋亡(与对照组相比,P<0.05)。因此,如无特别说明,以下实验均选择 10 μM Buparlisib (NVP-BKM120) 和 24 小时治疗。Buparlisib (NVP-BKM120) 治疗会导致所有测试的 MM 细胞系出现剂量依赖性生长抑制。Buparlisib (NVP-BKM120) IC50 因测试的 MM 细胞而异。在 24 小时治疗中,ARP-1、ARK 和 MM.1R 的 IC50 在 1 至 10 μM 之间,而 MM.1S 的 IC50 为 <1 μM,U266 的 IC50 在 10 至 100 μM 之间。总之,NVP-BKM120 治疗会导致 MM 细胞生长抑制和凋亡,且呈剂量和时间依赖性[2]

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

    体内研究
    (In Vivo)

    在 A2780 异种移植肿瘤中,口服 3、10、30、60 和 100 mg/kg Buparlisib (NVP-BKM120) 会导致 pAKTSer473 发生剂量依赖性调节。在 3 和 10 mg/kg 剂量下观察到 pAKTSer473 的部分抑制,在 30、60 或 100 mg/kg 剂量下观察到接近完全的抑制。pAKT 的抑制(以总 AKT 为标准)与血浆和肿瘤药物暴露量均有很好的跟踪[1]。接受 Buparlisib (NVP-BKM120)(每天每公斤 5 μM,持续 15 天)治疗的小鼠的肿瘤负担明显小于对照小鼠,以肿瘤体积(P<0.05)和循环人类 κ 链水平(P<0.05)来衡量。此外,NVP-BKM120 治疗显著延长了荷瘤小鼠的生存期(P<0.05)[2]

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

    Clinical Trial
    NCT NumberSponsorConditionStart DatePhase
    NCT01633060Novartis Pharmaceuticals|Novartis
    Metastatic Breast Cancer
    October 3, 2012Phase 3
    NCT01820325Novartis Pharmaceuticals|Novartis
    Non-Small Cell Lunch Cancer
    September 9, 2013Phase 1
    NCT01363232Array Biopharma, now a wholly owned subsidiary of Pfizer|Array BioPharma
    Advanced Solid Tumors|Selected Solid Tumors
    August 2011Phase 1
    分子量

    410.39

    Formula

    C18H21F3N6O2

    CAS 号
    性状

    固体

    颜色

    White to off-white

    中文名称

    布帕尼西

    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 (243.67 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)

    H2O 中的溶解度 : < 0.1 mg/mL (insoluble)

    配制储备液
    浓度 溶剂体积 质量 1 mg 5 mg 10 mg
    1 mM 2.4367 mL 12.1835 mL 24.3671 mL
    5 mM 0.4873 mL 2.4367 mL 4.8734 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    40% PEG300    5% Tween-80    45% Saline

      Solubility: ≥ 2.5 mg/mL (6.09 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。

      1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;再向上述体系中加入 50 μL Tween-80,混合均匀;然后再继续加入 450 μL 生理盐水 定容至 1 mL

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

      请依序添加每种溶剂: 10% DMSO    90% (20% SBE-β-CD in Saline)

      Solubility: ≥ 2.5 mg/mL (6.09 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。

      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 20% 的 SBE-β-CD 生理盐水水溶液 中,混合均匀。

      2 g SBE-β-CD(磺丁基醚 β-环糊精)粉末定容于 10 mL 的生理盐水中,完全溶解至澄清透明。

    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: 50% PEG300    50% Saline

      Solubility: 2.08 mg/mL (5.07 mM); 悬浊液; 超声助溶

    扫码获得
    动物溶解方案

    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 PEG300/PEG400Tween 80,均可在 MCE 网站选购。
    纯度 & 产品资料

    纯度: 99.90%

    参考文献
    Cell Assay
    [1]

    A2780 cells are cultured in DMEM supplemented with 10% FBS. L-glutamine, sodium pyruvate, and antibiotics. Cells are plated in the same medium at a density of 1000 cells per well, 100 uL per well into black-walled-clear-bottom plates and incubated for 3-5 hours. Buparlisib (NVP-BKM120) supplied in DMSO (20 mM) are diluted further into DMSO (7.5 uL of 20 mM Buparlisib (NVP-BKM120) in 22.5 uL DMSO. Mix well, transfer 10 uL to 20 uL DMSO, repeat until 9 concentrations have been made). The diluted Buparlisib (NVP-BKM120) solution (2 uL), is then added to cell medium (500 uL) cell medium. Equal volumes of this solution (100 uL) are added to the cells in 96 well plates and incubated at 37ºC for 3 days and developed using Cell Titer Glo. Inhibition of cell proliferation is determined by luminescence read using Trilux[1].

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

    Animal Administration
    [2]

    Mice[2]
    Six- to eight-week-old female severe combined immunodeficiency (SCID) mice are used. SCID mice are subcutaneously inoculated in the right flank with 1 million ARP-1 or MM.1S cells suspended in 50 μL phosphate-buffered saline (PBS). After palpable tumor developed (tumor diameter ≥5 mm), mice are treated with intraperitoneal injection of DMSO/PBS or Buparlisib (NVP-BKM120) (5 μM per kg per day) for 15 days. Tumor sizes are measured every 5 days, and blood samples are collected at the same period. Tumor burdens are evaluated by measuring tumor size and detecting circulating human kappa chain or lambda chain.

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

    参考文献

    完整储备液配制表

    * 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
    储备液的保存方式和期限:-80°C, 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 2.4367 mL 12.1835 mL 24.3671 mL 60.9177 mL
    5 mM 0.4873 mL 2.4367 mL 4.8734 mL 12.1835 mL
    10 mM 0.2437 mL 1.2184 mL 2.4367 mL 6.0918 mL
    15 mM 0.1624 mL 0.8122 mL 1.6245 mL 4.0612 mL
    20 mM 0.1218 mL 0.6092 mL 1.2184 mL 3.0459 mL
    25 mM 0.0975 mL 0.4873 mL 0.9747 mL 2.4367 mL
    30 mM 0.0812 mL 0.4061 mL 0.8122 mL 2.0306 mL
    40 mM 0.0609 mL 0.3046 mL 0.6092 mL 1.5229 mL
    50 mM 0.0487 mL 0.2437 mL 0.4873 mL 1.2184 mL
    60 mM 0.0406 mL 0.2031 mL 0.4061 mL 1.0153 mL
    80 mM 0.0305 mL 0.1523 mL 0.3046 mL 0.7615 mL
    100 mM 0.0244 mL 0.1218 mL 0.2437 mL 0.6092 mL
    Help & FAQs
    • 做细胞实验的时候,发现用 PBS 稀释母液之后就析出了是怎么回事呢?怎么处理呢?

      Buparlisib 的水溶性是不好的,所以如果您用 PBS 稀释的时候浓度比较大的话是可能会析出的,做细胞实验稀释建议您直接用培养基稀释到工作液的浓度,不建议用 PBS 稀释成中间梯度,同时用培养基稀释之后建议使用超声的方式促进溶解,确保完全澄清之后再换液加到培养板中进行培养。

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    目录号:
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