PD166866

PD166866 is a potent and selective small molecule inhibitor of fibroblast growth factor receptor 1 (FGFR1), demonstrating nanomolar affinity (IC50 ≈ 52–55 nM) as an ATP-competitive antagonist of the receptor tyrosine kinase. It is highly selective for FGFR1 over related kinases including PDGFR, EGFR, c-Src, MEK, PKC, and the insulin receptor tyrosine kinase. PD166866 inhibits FGFR1 autophosphorylation and downstream phosphorylation of mitogen-activated protein kinase (MAPK), resulting in suppression of FGF-induced but not EGF- or PDGF-induced cell proliferation. The compound exhibits antiangiogenic activity by inhibiting microvessel outgrowth from human placental arteries and shows anti-proliferative effects in cancer cell line models, promoting apoptosis. It is primarily investigated as an antineoplastic and angiogenesis inhibitor, with possible utility in fibrotic proliferative diseases and cartilage degeneration models[1][2][3][4][5][7][10][12].

Brand names

PD166866PD-166866PD 166866

Other names

1-(2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)-3-(tert-butyl)ureatert-butyl (2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl)carbamateN-[2-amino-6-(3,5-dimethoxyphenyl)pyrido[2,3-d]pyrimidin-7-yl]-N'-(1,1-dimethylethyl)FGF Receptor Tyrosine Kinase InhibitorFGF Receptor Tyrosine Kinase Inhibitor - CAS 192705-79-6 - Calbiochem