KRASG12C IN-18 is an orally active covalent KRAS G12C inhibitor that achieves complete covalent engagement of KRAS G12C in both GDP- and GMPPNP-bound states and displays strong antiproliferative activity against KRAS G12C and resistance-associated variants, including KRAS G12C/R68S , with low-nanomolar IC 50 values. KRASG12C IN-18 exhibits marked in vivo efficacy in KRAS G12C -driven solid tumor and KRAS G12C/R68S xenograft models and can be used for colorectal cancer research.
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