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

Chemical Structure : Poloppin II

CAS No.: 2248068-54-2

Poloppin II (Poloppin-II)

货号: PC-61201Not For Human Use, Lab Use Only.

Poloppin II is an orally active, Poloppin derivative inhibitor of protein-protein interaction via the PBD of the mitotic Polo-like kinase (PLK) with IC50 of 41 uM in FP assays, exhibits IC50 of 61 nM cellular assay for mitotic arrest.

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

    生物&药学活性

    Poloppin II is an orally active, Poloppin derivative inhibitor of protein-protein interaction via the PBD of the mitotic Polo-like kinase (PLK) with IC50 of 41 uM in FP assays, exhibits IC50 of 61 nM cellular assay for mitotic arrest。
    Poloppin II is also active against PLK2 PDB with an IC50 of 105 uM in FP assay, engages PLK1 and PLK4, sensitizes cells expressing mutant KRAS by approximately 5-fold。
    Poloppin II demonstrates effectivity gainst KRAS-expressing cancer xenografts.

    物理化学性质&存储条件

    分子量 511.973
    分子式 C28H25ClF3N3O
    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

    4-(5-(4-chlorophenyl)-1-(2-(trifluoromethyl)phenyl)-1H-pyrrol-2-yl)-N-(2-(dimethylamino)ethyl)benzamide

    参考文献

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

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