Fulzerasib

SKU: orb2567326

Description

Fulzerasib is an oral, covalent KRAS G12C inhibitor with potent activity against mutant tumor cell lines, demonstrating IC50 values in the low nanomolar range. It is a key research tool for investigating KRAS-driven oncogenesis and is utilized in both in vitro and in vivo studies for non-small cell lung cancer (NSCLC) and other solid tumors harboring the G12C mutation.

Research Area

Pharmacology & Drug Discovery, Signal Transduction

Key Properties

• CAS Number: 2641747-54-6
• MW: 617.07
• Purity: 99.22% (May vary between batches)
• Formula: C₃₂H₃₀ClFN₆O₄
• SMILES: O=C(C=C)N1CCN2C=3C=4C=C(Cl)C(=NC4N(C(=O)C3N(C(=O)C2C1)C)C=5C(=NC=CC5C)C(C)C)C=6C(F)=CC=CC6O
• Target: Ras,Kras
• Solubility: DMSO:100 mg/mL (162.06 mM)

Bioactivity

• In Vivo:
  Method: The antitumor activity of Fulzerasib was evaluated in pancreatic cancer cell line xenograft models (MIA Paca-2 CDX), human lung adenocarcinoma xenograft models (NCI-H358 CDX), patient-derived colon adenocarcinoma xenograft models (SW837 CDX), and patient-derived lung cancer xenograft models (LU2529 PDX). Result: Fulzerasib demonstrated potent antitumor activity in multiple xenograft models of pancreatic cancer, lung adenocarcinoma, and colon cancer.
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• In Vitro:
  Method: The mechanism of action of Fulzerasib on KRAS G12C was evaluated through in vitro enzymatic and cellular assays. The compound's ability to inhibit GDP/GTP nucleotide exchange (IC₅₀), reduce RAS-GTP levels (IC₅₀), and suppress downstream signaling molecule pERK (IC₅₀) was assessed. Additionally, its antiproliferative activity was tested in tumor cell lines harboring the KRAS G12C mutation. Result: Fulzerasib covalently inhibited GDP/GTP exchange on KRAS G12C (IC₅₀: 29 nM), locking KRAS in its inactive GDP-bound state (RAS-GTP IC₅₀: 74 nM) and blocking downstream signaling (pERK IC₅₀: 37 nM). Moreover, Fulzerasib effectively inhibited the proliferation of KRAS G12C-mutant tumor cell lines with IC₅₀ values ranging from 2 to 20 nM.
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Storage & Handling

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

Alternative Names

GFH 925, , ,

Compound Identifiers

PubChem CID

156732294