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

Chemical Structure : Tudociclib

CAS No.: 2640038-22-6

Tudociclib (INCB123667, INCB-123667)

货号: PC-27510Not For Human Use, Lab Use Only.

Tudociclib (INCB123667) is a potent and selective, orally available small molecule inhibitor of CDK2 with IC50 of <20 nM, is inactive against CDK1, CDK4, CDK6, CDK7, and CDK9.

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

    生物&药学活性

    Tudociclib (INCB123667) is a potent and selective, orally available small molecule inhibitor of CDK2 with IC50 of <20 nM, is inactive against CDK1, CDK4, CDK6, CDK7, and CDK9.
    INCB123667 inhibits phosphorylation of retinoblastoma (Rb), a CDK2/cyclin E substrate and key regulator of the G1-S transition.
    INCB123667 inhibits the expression of cell cycle regulatory genes in cyclin E-overexpressed cancer cells.
    INCB123667 resulted in G1 cell cycle arrest and cell senescence in ceullar assays.
    INCB123667 inhibits Rb phosphorylation and resulted in dose-dependent tumor growth inhibition along with minimal body weight loss in OVCAR3 tumor xenograft model.

    物理化学性质&存储条件

    分子量 419.50
    分子式 C18H25N7O3S
    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

    8-ethoxy-N-((3R,4S)-3-methyl-1-(methylsulfonyl)piperidin-4-yl)-7-(1H-pyrazol-4-yl)-[1,2,4]triazolo[1,5-a]pyridin-2-amine

    参考文献

    1. S. Wee, et al. European Journal of Cancer. Volume 174, Supplement 1S79October 2022

    2. Patent WO2021072232 A1 2021-04-15.

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