体外研究
PD-089828 (0.5-20 µM; 2 hours) inhibits PDGFR autophosphorylation with an IC
50
of 0.82 µM.
PD-089828 (1-50 µM; 2 hours) inhibits EGFR autophosphorylation with an IC
50
value of 10.9 µM.
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC
50
value of 0.63 µM.
PD-089828 (10 µM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC
50
value of 1.8 µM.
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC
50
values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 µM for bFGF-induced mitogenesis.
Cell Proliferation Assay
Cell Line:
Vascular smooth muscle cells (serum-stimulated growth)
Concentration:
10 µM
Incubation Time:
8 consecutive days
Result:
Produced a concentration-related inhibition of serum-stimulated cell growth with an IC50 value of 1.8 µM.
Western Blot Analysis
Cell Line:
Vascular smooth muscle cells (stimulated with PDGF-BB 30 ng/ml)
Concentration:
0.5-20 µM
Incubation Time:
2 hours
Result:
Inhibited PDGFR autophosphorylation with an IC
50
of 0.82 µM.
