RM-046 is an orally active, selective ternary complex inhibitor of KRAS Q61H (active form). RM-046 forms a ternary complex with cyclophilin A , binds to active KRAS Q61H in a non-covalent manner, blocks effector binding via steric hindrance and inhibits downstream signal transduction. RM-046 inhibits ERK phosphorylation and cancer cell proliferation, and induces sustained RAS pathway signal inhibition, anti-tumor activity and tumor regression in preclinical xenograft models. RM-046 can be used for the research of KRAS Q61H mutant cancers.
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