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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-Polo-like Kinase (PLK)-Poloppin
Poloppin

Chemical Structure : Poloppin

CAS No.: 683808-78-8

Poloppin

货号: PC-61200Not For Human Use, Lab Use Only.

Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.

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

    生物&药学活性

    Poloppin is a cell-active, small molecule inhibitor of protein-protein interaction via the Polo-box domain (PBD) of the mitotic Polo-like kinase (PLK) with IC50 of 26.9 uM (PLK1) in FP assays.
    Poloppin triggers dose-dependent mitotic arrest with non-congressed chromosomes in human cell lines, preferentially kills cells expressing mutant KRAS (SW48 G12D GI50=5.2 uM, SW48 Wt GI50=13.7 uM).
    Poloppin sensitizes mutant KRAS-expressing cells to clinical inhibitors of c-MET.

    物理化学性质&存储条件

    分子量 438.244
    分子式 C20H15BrF3NO2
    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

    3-(5-(4-bromophenyl)-1-(2-(trifluoromethyl)phenyl)-1H-pyrrol-2-yl)propanoic acid

    参考文献

    1. Narvaez AJ, et al. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7.

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