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ZSQ836

Chemical Structure : ZSQ836

CAS No.: 2634811-35-9

ZSQ836 (ZSQ 836)

Catalog No.: PC-49260Not For Human Use, Lab Use Only.

ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.

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    Biological Activity

    ZSQ836 (ZSQ 836) is a potent, selective and orally bioavailable CDK12/CDK13 covalent inhibitor with IC50 of 32 nM (CDK12), covalently interacts with Cys1039 of CDK12.
    ZSQ836 shows weak affinity (CDK9, GSK3A, and GSK3B) against a panel of 373 other kinases, exhibits comparable selectivity of organoarsenic CDK12/CDK13 covalent inhibitors to THZ531.
    ZSQ836 is a potent antagonist against ovarian cancer, provokes DNA damage in ovarian cancer.
    ZSQ836 is orally bioavailable and impairs tumor growth in vivo, and is efficacious in a murine ovarian tumor model.
    ZSQ836 suppresses T cell proliferation and activation.

    Physicochemical Properties

    M.Wt 627.054
    Formula C27H28AsClN6OS2
    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

    (R)-N-(4-(1,3,2-dithiarsolan-2-yl)phenyl)-2-(3-((5-chloro-4-(1H-indol-3-yl)pyrimidin-2-yl)amino)piperidin-1-yl)acetamide

    References

    1. Lin Cheng, et al. Cancer Res. 2022 Jul 20;CAN-22-0222.

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