Discovery and Characterization of Divarasib (GDC-6036), a Potent Covalent Inhibitor of KRAS G12C - PubMed
8 hours ago
- #covalent inhibitor
- #nonsmall cell lung cancer
- #KRAS G12C
- Divarasib (GDC-6036) is a potent, selective, and orally available covalent inhibitor of KRAS G12C.
- KRAS G12C is a prevalent oncogenic mutation in nonsmall cell lung cancer.
- Divarasib exhibits significant noncovalent binding, enhancing its potency and rapid kinetics.
- It shows superior potency and faster alkylation kinetics compared to other KRAS G12C inhibitors in vitro.
- Demonstrates robust tumor growth inhibition in KRAS G12C-positive cell lines.