Compound class:
Synthetic organic
Comment: RMC-6291 is a KRASG12C(ON) inhibitor [1], that inhibits active, GTP-bound RAS. It is designed to bind to the immunophilin cyclophilin A (PPIA) via a moiety containing a minimal cyclophilin A-binding motif of the naturally ocurring immunosuppressive (cyclophilin inhibiting) polyketide Sanglifehrin A. It also contains a cysteine-reactive warhead to mediate covalent tethering to KRAS. The resulting RMC-6291:cyclophilin A structure has high affinity for the active state of KRASG12C and forms a RMC-6291:cyclophilin A:KRASG12C tri-complex that causes steric hindrance for RAS effector binding thus blocking oncogenic signalling. The chemical structure of RMC-6291 was disclosed during the 'First Disclosures of New Drug Candidates' session at the April 2023 meeting of the AACR in Orlando. RMC-6291 was developed for anti-tumour potential.
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