MRTX849

MRTX849 is a potent (IC50’s = 14 nM NCI-H358; 5 nM MIA PaCa-2) and selective (over 463 proteins @ 1 µM) covalent KRASG12C inhibitor.1 It showed pronounced tumor regression in 17 of 26 KRASG12C-positive cell lines and xenograft models from multiple tumor types.2 MTRTX849 reversed the immunosuppressive tumor environment in a genetically modified mouse model and sensitized tumors to checkpoint inhibitor therapy in a genetically modified mouse KRASG12C lung adenocarcinoma model.3 It reversed ABCB1-mediated multidrug resistance in vitro and in vivo via attenuating ABCB1 efflux in drug-resistant cancer cells.4

Unconjugated

White solid

-20°C