Elironrasib is an orally active and covalent inhibitor of KRAS G12C (ON) . Elironrasib forms a tri-complex within tumor cells between KRAS G12C (ON) and cyclophilin A (CypA). Thus, Elironrasib prevents KRAS G12C (ON) from signaling via steric blockade of RAS effector binding. Elironrasib inhibits ERK signaling and induced apoptosis in KRASG12C-mutant H358 cells. Elironrasib also inhibits the proliferation of KRAS G12C mutant cells with a median IC 50 of 0.11 nM.
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