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CH-2-77

Chemical Structure : CH-2-77

CAS No.: 2408642-05-5

CH-2-77

Catalog No.: PC-38803Not For Human Use, Lab Use Only.

CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo.

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    Biological Activity

    CH-2-77 is a potent colchicine-binding site inhibitor (CBSI) targeting tubulin, shows potent anti-proliferative activity against a panel of cancer cells in vitro and efficacious anti-tumor effects in vivo.
    CH-2-77 inhibits the proliferation of both paclitaxel-sensitive and paclitaxel-resistant TNBC cells with an average IC50 of 3 nM.
    CH-2-77 also efficiently disrupts the microtubule assembly, inhibits the migration and invasion of TNBC cells, and induces G2/M cell cycle arrest.
    CH-2-77 shows acceptable overall pharmacokinetics and strongly suppresses the growth of orthotopic MDA-MB-231 xenografts without gross cumulative toxicities.
    CH-2-77 prevents lung metastasis originating from the mammary fat pad in a dose-dependent manner.

    Physicochemical Properties

    M.Wt 379.412
    Formula C22H21NO5
    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

    (6-(3-hydroxy-4-methylphenyl)pyridin-2-yl)(3,4,5-trimethoxyphenyl)methanone

    References

    1. Hao Chen, et al. J Med Chem. 2021 Aug 26;64(16):12049-12074.

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