PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 μM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 μM).
CAS:179343-17-0
分子式:C18H18Cl2N6O
分子量:405.3
纯度:98%
存储:Store at -20°C
Background:
PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM). It is selective for these targets over insulin receptor tyrosine kinase, PKC, and CDK4 (IC50s = >50 µM) but does inhibit MAPK (IC50 = 7.1 µM). PD 089828 decreases PDGF-BB-, EGF-, and bFGF-induced phosphorylation of PDGFR, EGFR, and FGFR1, respectively, in a concentration-dependent manner in vitro. It also decreases serum-stimulated growth (IC50 = 1.8 µM after 8 days) and migration (IC50 = 4.5 µM) of rat aortic smooth muscle cells.