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Substance Name: Naquotinib mesylate [USAN]
RN: 1448237-05-5
UNII: 12T09LV21O


  • NCI: 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. As this agent is selective towards mutant forms of EGFR, its toxicity profile may be reduced as compared to non-selective EGFR inhibitors which also inhibit wild-type EGFR. (NCI Thesaurus)

Molecular Formula

  • C30-H42-N8-O3.C-H4-O3-S

Molecular Weight

  • 658.8204

Classification Code

  • Treatment of Advanced Non-Small Cell Lung Cancer
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Names and Synonyms

Name of Substance

  • Naquotinib mesylate [USAN]


  • 6-Ethyl-3-((4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)phenyl)amino)-5-(((3R)-1-(1-oxoprop-2-en-1-yl)pyrrolidin-3-yl)oxy)pyrazine-2-carboxamide monomethanesulfonate
  • 6-Ethyl-3-(4-(4-(4-methylpiperazin-1-yl)piperidin-1-yl)anilino)-5-(((3R)-1-(prop-2-enoyl)pyrrolidin-3-yl)oxy)pyrazine-2-carboxamide monomethanesulfonate
  • ASP8273 mesilate
  • Naquotinib mesylate
  • UNII-12T09LV21O

Systematic Name

  • 2-Pyrazinecarboxamide, 6-ethyl-3-((4-(4-(4-methyl-1-piperazinyl)-1-piperidinyl)phenyl)amino)-5-(((3R)-1-(1-oxo-2-propen-1-yl)-3-pyrrolidinyl)oxy)-, methanesulfonate (1:1)

Registry Numbers

CAS Registry Number

  • 1448237-05-5


  • 12T09LV21O

System Generated Number

  • 1448237055

Structure Descriptors