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KRAS G12C inhibitor 11

Chemical Structure : KRAS G12C inhibitor 11

CAS No.: 2158297-63-1

KRAS G12C inhibitor 11

Catalog No.: PC-35953Not For Human Use, Lab Use Only.

KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM.

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    Biological Activity

    KRAS G12C inhibitor 11 is a potent, selective, covalent and irreversible inhibitor of KRAS G12C, inhibits KRAS dependent ERK-phosphorylation in the H358 cell with IC50 of 5 nM.
    KRAS G12C inhibitor 11 demonstrates super proportional dose ascending oral exposure in mice with 3h target coverage at the 30 mg/kg dose.
    KRAS G12C inhibitor 11 shows rapid growth inhibition and durable efficacy even after dosing was stopped, orally active.

    Physicochemical Properties

    M.Wt 551.695
    Formula C32H37N7O2
    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

    2-((S)-1-acryloyl-4-(2-(((S)-1-methylpyrrolidin-2-yl)methoxy)-7-(naphthalen-1-yl)-5,6,7,8-tetrahydropyrido[3,4-d]pyrimidin-4-yl)piperazin-2-yl)acetonitrile

    References

    1. U.S. Pat. Appl. Publ. (2018), US 20180072723 A1 20180315.

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