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首页-小分子抑制剂&激动剂-Apoptosis-Bcl-2-BM-1197
BM-1197

Chemical Structure : BM-1197

CAS No.: 1391107-89-3

BM-1197 (BM1197)

货号: PC-49799Not For Human Use, Lab Use Only.

BM-1197 (BM1197) is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL with Ki of < 1 nM, >1,000-fold selectivity over Mcl-1.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    BM-1197 (BM1197) is a potent and efficacious dual inhibitor of Bcl-2 and Bcl-xL with Ki of < 1 nM, >1,000-fold selectivity over Mcl-1.
    BM-1197 induces mechanism-based apoptosis in Mcl1-deficient mouse embryonic fibroblast (MEF) cells.
    BM-1197 disrupts the association between BCL-XL and PUMA, induces BAX translocation and cytochrome c release and BAX/BAK-dependent apoptosis in MEF/MCL1 −/− cells.
    BM-1197 exerts potent growth-inhibitory activity against small cell lung cancer (SCLC) cells in vitro (H146, IC50=3 nM).
    BM-1197 IV daily at 10 mg/kg (5 days per week for 2 weeks) exhibited antitumor efficacy in SCID mice bearing H146 or H1963 cells.

    物理化学性质&存储条件

    分子量 1131.77
    分子式 C53H59ClF4N6O7S4
    外观性状 Solid
    CAS No.
    储存条件
    固体粉末
    -20°C 12 个月; 4°C 6 个月
    配置液
    -80°C 6 个月; -20°C 6 个月
    Shipping
    Solubility

    10 mM in DMSO

    Chemical Name/SMILES

    N-[4-[4-[3-[2-(4-Chlorophenyl)-5-methyl-1-(1-methylethyl)-4-(methylsulfonyl)-1H-pyrrol-3-yl]-5-fluorophenyl]-1-piperazinyl]phenyl]-4-[[(1R)-3-(4-hydroxy-1-piperidinyl)-1-[(phenylthio)methyl]propyl]amino]-3-[(trifluoromethyl)sulfonyl]benzenesulfonamide

    参考文献

    1. Longchuan Bai, et al. PLoS One. 2014 Jun 5;9(6):e99404.

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