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Poloppin II

Chemical Structure : Poloppin II

CAS No.: 2248068-54-2

Poloppin II (Poloppin-II)

Catalog No.: 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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    Biological Activity

    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.

    Physicochemical Properties

    M.Wt 511.973
    Formula C28H25ClF3N3O
    Appearance Solid
    CAS No.
    Storage
    Solide Powder
    -20 °C 12 Months; 4°C 6 Months
    In Solvent
    -80 °C 6 Months; -20°C 6 Months
    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

    References

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

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