Naquotinib mesylate

  • Chemical Properties
CAS No. 1448237-05-5 Cat. No. BCP18906
Name Naquotinib mesylate
Synonyms ASP8273; ASP-8273; ASP 8273;
Formula C31H46N8O6S M. Wt 658.81
  • Biological Activity
Description Naquotinib mesylate is an orally available, mutant-selective and irreversible EGFR inhibitor; with IC50s of 8-33 nM toward EGFR mutants and 230 nM for EGFR.Naquotinib, also known as ASP8273, is an orally available, irreversible, third-generation, mutant-selective, epidermal growth factor receptor (EGFR) inhibitor with potential antineoplastic activity. Upon oral administration, ASP8273 covalently binds to and inhibits the activity of mutant forms of EGFR, including the T790M EGFR mutant, thereby preventing EGFR-mediated signaling. This may both induce cell death and inhibit tumor growth in EGFR-overexpressing tumor cells. EGFR, a receptor tyrosine kinase mutated in many tumor cell types, plays a key role in tumor cell proliferation and tumor vascularization. ASP8273 preferentially inhibits mutated forms of EGFR including T790M, a secondarily acquired resistance mutation, and may have therapeutic benefits in tumors with T790M-mediated resistance when compared to other EGFR tyrosine kinase inhibitors.
Pathways Angiogenesis/Protein Tyrosine Kinase Jak/Stat Pathway 
Targets EGFR 

Structure

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