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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-CDDD11-8
CDDD11-8

Chemical Structure : CDDD11-8

CAS No.: 2241659-94-7

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CDDD11-8 (CDDD 11-8)

货号: PC-21462Not For Human Use, Lab Use Only.

CDDD11-8 is a potent, selective, orally bioavailable CDK9 inhibitor with Ki of 8 nM, shows >50-fold selectivity over other CDKs, also inhibits FLT3-ITD with Ki of 13 nM.

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

    生物&药学活性

    CDDD11-8 is a potent, selective, orally bioavailable CDK9 inhibitor with Ki of 8 nM, shows >50-fold selectivity over other CDKs, also inhibits FLT3-ITD with Ki of 13 nM.
    CDDD11-8 also inhibits TRKC, FLT3, NUAK1, GLK, MINK, TNIK, and MST1 with Ki of 10 to 46 nM in a panel of 369 human kinases.
    CDDD11-8 exhibits potent anti-proliferative effects leukemic cells that harbored the FLT3-ITD mutation and MLL fusions, such as MV4-11 (FLT3ITD/ITD/MLL-AF4) and MOLM-13 (FLT3ITD/WT/MLL-AF9), and those driven by TRK fusions (e.g., MO91) with GI50 values of < 0.1 uM.
    CDDD11-8 (1 µM) decreases the level of total RNAP II and tubulin, suppresses the expressions of c-MYC, MCL-1, and XIAP in MV4-11 and MOLM-13 cells.
    CDDD11-8 (75 and 125 mg/kg, PO, QD) demonstrates tumor growth inhibition efficacy against MV4-11 tumor xenografts.
    CDDD11-8 also has efficacy in TNBC without apparent toxicity to normal tissues.

    物理化学性质&存储条件

    分子量 398.51
    分子式 C24H26N6
    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

    (1r,4r)-N1-(5-methyl-4-(6-phenylimidazo[1,2-a]pyridin-3-yl)pyrimidin-2-yl)cyclohexane-1,4-diamine

    参考文献

    1. Abel Tesfaye Anshabo, et al. Cancers (Basel). 2022 Feb 22;14(5):1113.

    2. Mustafa EH, et al. Oncogene. 2023 Nov 24. doi: 10.1038/s41388-023-02892-3.

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