2922732-54-3

Product Details:

CasNo： 2922732-54-3

Molecular Formula： C63H88F3N11O7

Appearance： White to off-white Powder

Packing： Aluminium bag

Throughput： 100KG/Month

Purity： 99%

Zoldonrasib (RMC‑9805) is an investigational, orally bioavailable, first‑in‑class RAS(ON) G12D‑selective covalent tri‑complex inhibitor discovered and developed by Revolution Medicines.

Distinct from conventional KRAS G12C inhibitors that target GDP‑bound inactive RAS, zoldonrasib acts via a unique tri‑complex mechanism of action. It first binds non‑covalently to cyclophilin A (CypA) to form a binary complex. This binary assembly then selectively recognizes the GTP‑bound, oncogenically active KRAS G12D mutant, and forms a stable tri‑complex with irreversible covalent engagement at the mutant aspartate residue. The newly formed tri‑complex sterically blocks the binding interface between KRAS G12D and downstream RAF effectors, thereby shutting down aberrant MAPK oncogenic signaling and suppressing tumour cell proliferation and survivalRevolution....

KRAS G12D represents the most prevalent RAS oncogenic alteration, accounting for approximately 29% of all RAS‑driven malignancies, including pancreatic ductal adenocarcinoma, non‑small cell lung cancer (NSCLC), colorectal carcinoma and other gastrointestinal tumours. For decades, KRAS G12D-positive cancers have lacked approved targeted therapeutic options, constituting a major unmet clinical need in oncologyRevolution....

Zoldonrasib has been granted FDA Breakthrough Therapy Designation for adult patients with KRAS G12D‑mutated locally advanced or metastatic NSCLC who have progressed following prior anti‑PD‑(L)1 immunotherapy and platinum‑based chemotherapy. Multiple global Phase 2 and Phase 3 pivotal trials (including RASolute and RASolve study programmes) are ongoing to evaluate zoldonrasib as monotherapy and in combination regimens across lung, pancreatic and other KRAS G12D‑mutated solid tumoursRevolution....

Disclaimer: Zoldonrasib is an investigational agent and has not yet received marketing approval in any jurisdiction. Safety and efficacy have not been fully established.