Catalog No.: PC-35878Not For Human Use, Lab Use Only.
KRAS G12C inhibitor 13 is a potnt, irreversible, covalent and in vivo-active inhibitor of KRAS-G12C, suppresses ERK phosphorylation with IC50 of 70 nM in H358 cell assays.
KRAS G12C inhibitor 13 is a potnt, irreversible, covalent and in vivo-active inhibitor of KRAS-G12C, suppresses ERK phosphorylation with IC50 of 70 nM in H358 cell assays.
KRAS-G12C inhibitor 13 displays no significant activity against non-G12C cell lines with IC50 of >16 uM.
KRAS-G12C inhibitor 13 demonstrates KRAS-G12C target engagement in vivo and antitumor efficacy in the MIA PaCa-2 tumor xenograft models.
1. Jay B. Fell, et al. Discovery of Tetrahydropyridopyrimidines as Irreversible Covalent Inhibitors of KRAS-G12C with In Vivo Activity. ACS Med. Chem. Lett. DOI: 10.1021/acsmedchemlett.8b00382.
