Preferred Label : Naquotinib;
NCIt synonyms : 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)-;
NCIt definition : 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.;
UNII : 47DD4548PB;
InChIKey : QKDCLUARMDUUKN-XMMPIXPASA-N;
CAS number : 1448232-80-1;
Molecule name : ASP8273;
NCI Metathesaurus CUI : CL472641;
Origin ID : C115110;
UMLS CUI : C4519293;
Currated CISMeF NLP mapping
Semantic type(s)
UMLS correspondences (same concept)
concept_is_in_subset