PD-089828

PD-089828 is an ATP competitive inhibitor of FGFR-1, PDGFR-β and EGFR (IC₅₀s=0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of c-Src tyrosine kinase (IC₅₀=0.18 µM). PD-089828 also inhibits MAPK with an IC₅₀ of 7.1 µM. PD-089828 inhibits PDGF-, EGF- and bFGF-mediated tyrosine kinase receptor autophosphorylation in vitro. PD-089828 has a long-lasting cellular activity^[1]. In Vitro: PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC₅₀ of 0.82 µM^[1].
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC₅₀ value of 10.9 µM^[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC₅₀ value of 0.63 µM^[1]. PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC₅₀ value of 1.8 µM^[1].
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC₅₀ values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis^[1].