RM-046

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.

• Data Sheet (276 KB)