KRASG12C IN-18 is a potent covalent inhibitor targeting the KRASG12C mutation. It effectively engages KRASG12C in both GDP- and GMPPNP-bound states, demonstrating significant antiproliferative activity against KRASG12C and its resistance variants, including KRASG12C/R68S, with low nanomolar IC50 values. This compound exhibits substantial in vivo efficacy in models of KRASG12C-driven solid tumors and KRASG12C/R68S xenografts, making it a valuable tool for research in colorectal cancer.
KRASG12C IN-18 is a potent covalent inhibitor targeting the KRASG12C mutation. It effectively engages KRASG12C in both GDP- and GMPPNP-bound states, demonstrating significant antiproliferative activity against KRASG12C and its resistance variants, including KRASG12C/R68S, with low nanomolar IC50 values. This compound exhibits substantial in vivo efficacy in models of KRASG12C-driven solid tumors and KRASG12C/R68S xenografts, making it a valuable tool for research in colorectal cancer.
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