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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-CRCM5484
CRCM5484

Chemical Structure : CRCM5484

CAS No.: 3022975-51-2

CRCM5484 (CRCM-5484)

货号: PC-72866Not For Human Use, Lab Use Only.

CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.

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

    生物&药学活性

    CRCM5484 is a potent, BET BDII-selective inhibitor with IC50 of 130/20/71 nM for BRD4-BD2/BRD3-BD2/BRD2-BD2, respectively.
    CRCM5484 displays 475-fold selectivity over its first bromodomain (BRD3-BD2 vs BRD3-BD1).
    CRCM5484 demonstrates very low activity in various cell-based assays.
    CRCM5484 modulates the anti-leukemic activity in combination with various FDA-approved and/or in-development drugs in a cell- and context-dependent differential manner.

    物理化学性质&存储条件

    分子量 509.599
    分子式 C24H23N5O4S2
    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

    2-((7-acetyl-3-(furan-2-ylmethyl)-4-oxo-3,4,5,6,7,8-hexahydropyrido[4',3':4,5]thieno[2,3-d]pyrimidin-2-yl)thio)-N-(2-methylpyridin-3-yl)acetamide

    参考文献

    1. Kendall Carrasco, et al. J Med Chem. DOI: 10.1021/acs.jmedchem.1c02168

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