An inhibitor of EGFR, PDGFβ, FGF, and c-Src
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.
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