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SNX631

Chemical Structure : SNX631

CAS No.: 868066-26-6

SNX631 (SNX-631)

Catalog No.: PC-49204Not For Human Use, Lab Use Only.

SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.

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    Biological Activity

    SNX631 (SNX-631) is a potent, selective inhibitor of CDK8/19 Mediator kinase with IC50 of 10.3 nM in the NF κB-dependent cell-based assays.
    SNX631 is 6 to 10 times more potent than Senexin B in all the assays except for the DiscoverX activesite-dependent competition binding assay.
    SNX631 showed synergistic interactions with lapatinib and trastuzumab in a panel of HER2+ BrCa cell lines, overcoming and preventing resistance to HER2-targeting drugs.
    Combination of HER2-mAb trastuzumab and SNX631 inhibited STAT1 and STAT3 phosphorylation at S727 and up-regulated tumor suppressor BTG2 in HER2+ BrCa cell lines.
    SNX631 partially inhibits growth of xenograft tumors formed by lapatinib-sensitive or -resistant HER2+ breast cancer cells alone, and strongly suppressed by the combination of lapatinib, overcoming lapatinib resistance.

    Physicochemical Properties

    M.Wt 438.550
    Formula C22H26N6O2S
    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-amino-4-(4-(4-(dimethylcarbamoyl)phenyl)-1,4-diazepan-1-yl)thieno[2,3-b]pyridine-2-carboxamide

    References

    1. Jing Li, et al. Cells. 2019 Oct 6;8(10):1208.

    2. Xiaokai Ding, et al. Proc Natl Acad Sci U S A. 2022 Aug 9;119(32):e2201073119.

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