MRTX849
Covalent KRASG12C inhibitor / 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
Biochemicals & reagents
2326521-71-3
Adagrasib
1) Fell et al. (2020), Identification of the Clinical Development Candidate MRTX849, a Covalent KRASG12C Inhibitor for the Treatment of Cancer; J. Med. Chem. 63 6679 2) Hallin et al. (2020); The KRASG12C Inhibitor, MRTX849, Provides Insight Toward Therapeutic Susceptibility of KRAS Mutant Cancers in Mouse Models and Patients, Cancer Discov., 10 54 3) Briere et al. (2021); The KRASG12C Inhibitor MRTX849 Reconditions the Tumor Immune Microenvironment and Sensitizes Tumors to Checkpoint Inhibitor Therapy, Mol. Cancer Ther., 20 975 4) Zhang et al. (2022); Adagrasib, a KRAS G12C inhibitor, reverses the multidrug resistance mediated by ABCB1 in vitro and in vivo, Cell Commun. Signal., 20 142
-20°C
TARGET: GTPase -- PATHWAY: ERK -- RESEARCH AREA: Immunology -- DISEASE AREA: Cancer