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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-BMS-641988
BMS-641988

Chemical Structure : BMS-641988

CAS No.: 573738-99-5

BMS-641988 (BMS 641988;BMS641988)

货号: PC-61086Not For Human Use, Lab Use Only.

BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM.

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

    生物&药学活性

    BMS-641988 is a potent, selective, nonsteroidal androgen receptor antagonist with Ki of 1.7 nM, MDA-MB-453 cell IC50 of 16 nM.
    BMS-641988 displays high selectivity over the glucocorticoid and progesterone receptors.
    BMS-641988 displayed 3-7-fold increased antagonist activity of AR transactivation compared with bicalutamide.
    BMS-641988 strongly inhibits androgen-dependent growth of the ventral prostate and seminal vesicles in rats, and is efficacious in CWR-22-BMSLD1 tumors initially refractory to treatment with bicalutamide.

    物理化学性质&存储条件

    分子量 471.45
    分子式 C20H20F3N3O5S
    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-((3aR,4R,5R,7R,7aS)-2-(4-cyano-3-(trifluoromethyl)phenyl)-4,7-dimethyl-1,3-dioxooctahydro-1H-4,7-epoxyisoindol-5-yl)ethanesulfonamide

    参考文献

    1. Balog A, et al. ACS Med Chem Lett. 2015 Jun 19;6(8):908-12.

    2. Attar RM, et al. Cancer Res. 2009 Aug 15;69(16):6522-30.

    3. Rathkopf D, et al. Clin Cancer Res. 2011 Feb 15;17(4):880-7.

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