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CDK7 and 9 inhibitor 14

Chemical Structure : CDK7 and 9 inhibitor 14

CAS No.: 851439-14-0

CDK7 and 9 inhibitor 14 (CDK7/9-IN-14)

Catalog No.: PC-61180Not For Human Use, Lab Use Only.

CDK7/9-IN-14 is a potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.

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

    Biological Activity

    CDK7/9-IN-14 is a potent, selective transcriptional CDK inhibitor with Ki of 2.3 and 0.38 nM for CDK7 and CDK9, respectively.
    CDK7/9-IN-14 displays >30-fold selectivity over CDK1/2/4, inhibits VEGFR2 with IC50 of 180 nM in a panel of non-CDK kinases.
    CDK7/9-IN-14 demonstrates a broad spectrum of in vitro antitumor activity with average IC50 of 0.3 uM with no selectivity toward cell line types based on p53, p21, p16, or pRb status.
    CDK7/9-IN-14 significantly reduces phosphorylation of both Ser-2 and Ser-5 of the RNAP-II CTD, reduces antiapoptotic protein levels in cells, and selectively induces apoptosis in transformed cells.
    CDK7/9-IN-14 demonstrates antitumor activity in murine xenograft solid tumor models.

    Physicochemical Properties

    M.Wt 382.486
    Formula C19H22N6OS
    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

    3,4-dimethyl-5-[2-(4-piperazin-1-yl-phenylamino)-pyrimidin-4-yl]-3H-thiazol-2-one

    References

    1. Wang S, et al. Chem Biol. 2010 Oct 29;17(10):1111-21.

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