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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-CG13250
CG13250

Chemical Structure : CG13250

CAS No.: 1629873-75-1

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CG13250 (CG250, CG 13250)

货号: PC-20160Not For Human Use, Lab Use Only.

CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).

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

    生物&药学活性

    CG13250 (CG 13250, CG250) is a potent, selective and orally bioavailable BET bromodomain inhibitor with Kd of 44 nM (BRD4), IC50 of 1.1 uM (BRD4 BD1+BD2).
    CG13250 inhibits the cell growth of MV4;11 cells with GI50 of 595 nM.
    CG13250 is very selective for the Group II bromodomain-containing proteins (BCPs), which are the BET proteins, inhibiting all of them -many completely- at 10 uM, also significantly inhibits BRD9, BRPF1, CREBBP and EP300.
    CG13250 displays high selectivity against 408 non-mutant kinases using DiscoverX's KINOMEscanTM platform.
    CG13250 inhibits the binding of BRD4 to c-MYC promoter regions suppressing the transcription of the c-MYC gene.
    CG13250 (25 mg/kg, PO, qD) prolongs the survival of in a subcutaneous murine model of a Kasumi-1 xenograft tumor for leukemia, with no body weight loss.

    物理化学性质&存储条件

    分子量 345.40
    分子式 C21H19N3O2
    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

    4-(benzylamino)-6-(3,5-dimethylisoxazol-4-yl)quinoline-2(1H)-one

    参考文献

    1. Jay Chauhan, et al. Bioorg Med Chem Lett. 2023 Mar 9;129220.

    2. Imayoshi N, et al. Biochem Biophys Res Commun. 2017 Mar 4;484(2):262-268.

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