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RMC-6236

CAS No.: 2765081-21-6
Product introduction:RMC-6236, also known as Daraxonrasib, is a first-in-class, oral, noncovalent RAS(ON) multi-selective tri-complex inhibitor developed by Revolution Medicines. Unlike conventional KRAS G12C inhibitors that target the inactive GDP-bound state, RMC-6236 targets the active GTP-bound state (RAS(ON)) of both mutant and wild-type RAS isoforms, including KRAS, NRAS, and HRAS. The compound forms a stable tri-complex with cyclophilin A and the GTP-bound RAS protein, potently blocking downstream signaling pathways essential for tumor growth. It has demonstrated promising clinical activity in patients with pancreatic ductal adenocarcinoma (PDAC) and other RAS-mutant solid tumors, representing a potential breakthrough for cancers historically considered "undruggable".

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CAS No.:2765081-21-6

RMC-6236 is a white to off-white solid powder with the molecular formula C₃₉H₄₂N₈O₃ and a molecular weight of approximately 670.81 g/mol. It is a bRo5 (beyond Rule of 5) molecule designed for oral bioavailability and potent RAS(ON) inhibition across multiple RAS variants. The compound is soluble in organic solvents such as DMSO and exhibits high binding affinity for GTP-bound RAS proteins. It is stable under recommended storage conditions (dry, cool, and protected from light). The 300 mg once-daily dose has been selected as the phase 3 dose based on clinical studies. The compound is currently available for research and clinical trial use only, with a purity specification typically ≥98% for investigational applications.

Core Functions:

  • Active investigational agent in Phase 3 clinical trials for previously treated metastatic pancreatic ductal adenocarcinoma (RASolute 302) 

  • Investigational therapy for first-line metastatic pancreatic cancer (RASolute 303) and adjuvant treatment in resectable PDAC (RASolute 304) 

  • Phase 3 clinical development in previously treated RAS-mutant non-small cell lung cancer (RASolve 301) 

  • Research use in RAS-driven oncology, including combination studies with tumor-treating fields and chemotherapy

  • Preclinical and clinical research in colorectal cancer and other RAS-addicted solid tumors

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