RMC5127

SKU: orb2945998

Description

RMC5127 is a brain-penetrant, oral inhibitor selectively targeting the KRAS G12V mutation. It blocks oncogenic RAS signaling, triggering apoptosis in mutant cells, and demonstrates antitumor efficacy in both cellular and animal models of KRAS G12V-driven cancers.

Research Area

Cell Biology, Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 3056146-38-1
• MW: 1062.32
• Purity: 99.96% (May vary between batches)
• Formula: C₅₇H₇₅N₉O₉S
• SMILES: C[C@H](OC)C(N=C1)=[C@@]([C@@]2=C(CC(C)(C)COC([C@H]3NN(C([C@@H](NC([C@H]4OC[C@@H]4C)=O)[C@H]5N6CC7(COC7)C6)=O)C8CC3C8)=O)C9=C(C=CC(C%10=CSC5=N%10)=C9)N2CCOC%11CCOCC%11)C=C1N%12CCN(C%13CC%13)CC%12
• Target: Kras,Kras,Apoptosis,Ras
• Solubility: DMSO:100 mg/mL (94.13 mM)

Bioactivity

• In Vivo:
  Following repeated oral administration of RMC5127 to subcutaneous cell line-derived xenograft (CDX) models and patient-derived xenograft (PDX) models of non-small cell lung cancer (NSCLC), pancreatic ductal adenocarcinoma (PDAC), and colorectal cancer (CRC) harboring the KRASG12V mutation, significant and durable antitumor activity was observed. In the whole brain tissues of naïve mice (tumor-free mice), dose-dependent exposure of RMC5127 was detected, indicating that this compound possesses blood-brain barrier penetration ability .
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• In Vitro:
  In a panel of human cancer cell lines harboring the KRASG12V mutation, RMC5127 significantly suppressed RAS pathway activity, inhibited cell proliferation, and induced cell apoptosis; however, in a panel of K/N/HRAS wild-type cancer cell lines, this drug only exerted a submaximal inhibitory effect .
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RMC-5127, RMC 5127

Compound Identifiers

PubChem CID

176455488