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IIIM-290

Chemical Structure : IIIM-290

CAS No.: 2213468-64-3

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IIIM-290 (IIIM290)

Catalog No.: PC-62534Not For Human Use, Lab Use Only.

IIIM-290 (IIIM290) is a potent, orally active cyclin-dependent kinase (CDK) inhiitor with IC50 of 1.9 and 16 nM for Cdk-9/T1 and Cdk-2/A, respectively.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

    Biological Activity

    IIIM-290 (IIIM290) is a potent, orally active cyclin-dependent kinase (CDK) inhiitor with IC50 of 1.9 and 16 nM for Cdk-9/T1 and Cdk-2/A, respectively.
    IIIM-290 selectively inhibits Molt-4/MIAPaCa-2 cell growth with GI50 of <1 uM.
    IIIM-290 inhibits the cell growth of MIAPaCa-2 cells via caspase-dependent apoptosis, demonstrates in vivo efficacy in pancreatic, colon, and leukemia xenografts at 50 mg/kg, po., without CYP/efflux-pump liability, and mutagenic/genotoxic or cardiotoxic effects.

    Physicochemical Properties

    M.Wt 462.323
    Formula C23H21Cl2NO5
    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

    (1'R,2'S)-2-(2,6-Dichlorostyryl)-5,7-dihydroxy-8-(3-hydroxy-1- methylpiperidin-4-yl)-4H-chromen-4-one

    References

    1. Bharate SB, et al. J Med Chem. 2018 Feb 22;61(4):1664-1687.

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