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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Cyclin-dependent Kinase (CDK)-RGB-286147
RGB-286147

Chemical Structure : RGB-286147

CAS No.: 784211-09-2

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RGB-286147 (RGB 286147)

货号: PC-49789Not For Human Use, Lab Use Only.

RGB-286147 (RGB 286147) is a proteome-wide CDK/CRK-specific kinase inhibitor with IC50 of 48 and 15 nM for CDK1/CycB and CDK2/CycE, respectively.

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

    生物&药学活性

    RGB-286147 (RGB 286147) is a proteome-wide CDK/CRK-specific kinase inhibitor with IC50 of 48 and 15 nM for CDK1/CycB and CDK2/CycE, respectively.
    RGB-286147 weakly inhibits CDK4/6 and GSK3b with IC50 of 839/282 and 754 nM, respectively.
    RGB-286147 inhibited the kinase activity of CDK3, CDK5, and CDK7, with similar potency (low nanomolar IC50 values, 10-70 nM).
    RGB-286147 also inhibited the autophosphorylation of CDK9 as well as the crossphosphorylation of cyclin T1 by CDK9 in a dose-dependent manner and with comparable potency.
    RGB-286147 is a potential CDK20 inhibitor.
    RGB-286147 caused a pronounced G1 arrest, endoreduplication, and apoptotic cell death in HCT116 cells, inhibited HCT116 cell viability with IC50 of 57 nM (24h).
    RGB-286147 is a highly potent and broad-spectrum inhibitor of tumor cell growth with average GI50 of <10 nM at 48 hr of exposure.

    物理化学性质&存储条件

    分子量 473.35
    分子式 C23H22Cl2N4O3
    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

    1-(2,6-dichlorophenyl)-6-(4-(2-hydroxyethoxy)benzyl)-3-isopropyl-1,5-dihydro-4H-pyrazolo[3,4-d]pyrimidin-4-one

    参考文献

    1. Maureen Caligiuri, et al. Chem Biol. 2005 Oct;12(10):1103-15.

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