1-(2-Amino-6-(3,5-dimethoxyphenyl)-pyrido(2,3-d)pyrimidin-7-yl)-3-tert-butyl urea

BeschreibungPD 166866 is a potent inhibitor of fibroblast growth factor receptor 1 (FGFR1; IC50 = 52.4 nM; Ki = 45.2 nM). It is selective for FGFR1 over PDGFR, EGFR, C-SRC, MEK, PKC, insulin receptor tyrosine kinase, and CDK4 (IC50s = >50 μM). PD 166866 inhibits FGFR1 autophosphorylation in NIH3T3 and L6 cells (IC50s = 10.8 and 3.1 nM, respectively) and inhibits phosphorylation of MAPK (IC50s = 4.3 and 7.9 nM for the 44- and 42-kDa MAPK isoforms, respectively). It reduces FGF- but not EGF- or PDGF-stimulated growth of L6 cells and inhibits microvessel outgrowth from human placental arteries in vitro. PD 166866 inhibits the growth of non-small cell lung cancer (NSCLC) cell lines in a dose-dependent manner and reduces migration of VL-8 cells at a concentration of 10 μM.

VerwendenA novel potent ATP competitive pyrido[2,3-d]pyrimidine tyrosine kinase inhibitors. An inhibitor of the basic fibroplast growth factor (bFGF).