AMG 510 is a potent (IC 50 ’s = 6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRAS G12C inhibitor. It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses. AMG 510 improved the efficacy...
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AMG 510 is a potent (IC 50 ’s = 6 nM NCI-H358; 9 nM MIA PaCa-2) covalent KRAS G12C inhibitor. It significantly inhibited tumor growth in NCI-H358 and MIA PaCa-2 cell lines as well as CT-26 tumors (mouse syngeneic model) and caused tumor regression at higher doses. AMG 510 improved the efficacy of various other chemotherapeutic agents including inhibitors of HER kinases, EGFR, SHP2, PI3K, AKT, and MEK and synergized with immune checkpoint reagents. FDA approved for use in KRAS G12C -positive non-small cell lung cancer. AMG 510 displayed efficacy alone and in combination with trametinib and/or buparlisib in pancreatic ductal adenocarcinoma cell lines
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