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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Checkpoint Kinase (Chk)-VER-158411
VER-158411

Chemical Structure : VER-158411

CAS No.: 1174664-88-0

VER-158411 (VER-00158411, V-158411)

货号: PC-60279Not For Human Use, Lab Use Only.

VER-158411 (V-158411) is a potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.

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

    生物&药学活性

    VER-158411 (V-158411) is a potent, selective, ATP-competitive Chk1 and Chk2 inhibitor with IC50 of 4.4 nM and 4.5 nM, respectively.
    VER-158411 dispalys >1,000-fold selectivity over CDK1.
    VER-158411 reduces pChk1 (S296) and pChk2 (S516) levels in a concentration dependent fashion in cells treated with etoposide with IC50s of 48 nM for Chk1 and 904 nM for Chk2.
    VER-158411 potentiates the cytotoxicity of chemotherapeutic agents in a variety of p53 deficient human tumor cell lines (GI50=0.5-9.5 uM) and human colon tumor xenograft models.

    物理化学性质&存储条件

    分子量 538.652
    分子式 C31H34N6O3
    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-benzyl-N-(5-(5-(3-(dimethylamino)-2,2-dimethylpropoxy)-1H-indol-2-yl)-6-oxo-1,6-dihydropyridin-3-yl)-1H-pyrazole-4-carboxamide

    参考文献

    1. Massey AJ, et al. Oncotarget. 2015 Nov 3;6(34):35797-812.

    2. Alsubhi N, et al. Mol Oncol. 2016 Feb;10(2):213-23.

    3. Wayne J, et al. Oncotarget. 2016 Dec 20;7(51):85033-85048.

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