Preferred Label : FGFR4 Inhibitor BLU 9931;
NCIt synonyms : N-(2-((6-(2,6-Dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl)amino)-3-methylphenyl)-2-propenamide; 2-Propenamide, N-(2-((6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-quinazolinyl)amino)-3-methylphenyl)-;
NCIt related terms : BLU-9931;
NCIt definition : An orally bioavailable, selective inhibitor of human fibroblast growth factor receptor
4 (FGFR4), with potential antineoplastic activity. Upon oral administration, FGFR4
antagonist BLU 9931 specifically and irreversibly binds to the cysteine residue at
position 552 (Cys 552) that is within the active site of FGFR4. This blocks FGFR4
autophosphorylation and activation of receptor tyrosine kinase activity that would
normally occur after binding to its ligand, fibroblast growth factor 19 (FGF19), which
both inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation
in FGF19- and FGFR4-overexpressing cells. FGFR4, a receptor tyrosine kinase, is involved
in angiogenesis and in the proliferation, differentiation, and survival of tumor cells.
FGFR4 expression is associated with poor prognosis. FGF19 is overexpressed by certain
tumor cell types.;
UNII : FQK825B5DX;
InChIKey : TXEBNKKOLVBTFK-UHFFFAOYSA-N;
CAS number : 1538604-68-0;
Molecule name : BLU 9931; BLU-9931;
NCI Metathesaurus CUI : CL970841;
Origin ID : C162342;
UMLS CUI : C4547345;
Currated CISMeF NLP mapping
- BLU9931 [MeSH Supplementary Concept]
- Semantic type(s)
- UMLS correspondences (same concept)
- BLU9931 [MeSH Supplementary Concept]
- concept_is_in_subset
