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ST-162

Chemical Structure : ST-162

CAS No.: 1883817-83-1

ST-162 (ST162)

Catalog No.: PC-61742Not For Human Use, Lab Use Only.

ST-162 is a potent, bifunctional MAPK/PI3K antagonist with IC50 of 191 nM and 398 nM for PI3Kα and MEK1, respectively.

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    Biological Activity

    ST-162 is a potent, bifunctional MAPK/PI3K antagonist with IC50 of 191 nM and 398 nM for PI3Kα and MEK1, respectively.
    ST-162 produces regression of mutant KRAS or BRAF addicted xenograft models of colorectal cancer and melanoma and stasis of BRAF/PTEN mutant melanomas.
    ST-162 increases efficacy in a syngeneic KRAS mutant colorectal cancer model combined with checkpoint blocker PD-L1.

    Physicochemical Properties

    M.Wt 982.752
    Formula C40H44F5IN10O6
    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

    N-(2-(2-(2-(2-(4-(4-(2-(difluoromethyl)-1H-benzo[d]imidazol-1-yl)-6-morpholino-1,3,5-triazin-2-yl)piperazin-1-yl)ethoxy)ethoxy)ethoxy)ethoxy)-3,4-difluoro-2-((2-fluoro-4-iodophenyl)amino)benzamide

    References

    1. Galbán S, et al. Mol Cancer Ther. 2017 Nov;16(11):2340-2350.

    2. Van Dort ME, et al. J Med Chem. 2016 Mar 24;59(6):2512-22.

    3. Van Dort ME, et al. ACS Med Chem Lett. 2017 Jul 24;8(8):808-813.

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