RM-041 is a selective, orally active inhibitor targeting KRAS[G13C](ON), forming a covalent complex with both KRASG13C (ON) and Cyclophilin A. This compound effectively blocks the binding of RAS effector proteins through steric hindrance and irreversibly binds to Cys-13, leading to the inhibition of KRASG13C mutant cancer cell proliferation. RM-041 demonstrates significant regression of KRASG13C tumors in both cellular and xenograft tumor models and exhibits a synergistic effect in combination with upstream inhibitors, such as SHP2 inhibitors. It serves as a valuable research tool in studying non-small cell lung cancer.
RM-041 is a selective, orally active inhibitor targeting KRAS[G13C](ON), forming a covalent complex with both KRASG13C (ON) and Cyclophilin A. This compound effectively blocks the binding of RAS effector proteins through steric hindrance and irreversibly binds to Cys-13, leading to the inhibition of KRASG13C mutant cancer cell proliferation. RM-041 demonstrates significant regression of KRASG13C tumors in both cellular and xenograft tumor models and exhibits a synergistic effect in combination with upstream inhibitors, such as SHP2 inhibitors. It serves as a valuable research tool in studying non-small cell lung cancer.
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