PD-161570 is a potent and ATP-competitive human FGF-1 receptor inhibitor with an IC50 of 39.9 nM and a Ki of 42 nM. PD-161570 also inhibits the PDGFR, EGFR and c-Src tyrosine kinases with IC50 values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibits PDGF-stimulated autophosphorylation and FGF-1 receptor phosphorylation with IC50s of 450 nM and 622 nM, respectively. PD-161570 is also a bone morphogenetic proteins (BMPs) and TGF-β signaling inhibitor.
体外研究
PD-161570 (Compound 6c; 0.1-1 µM; 1-8 days; VSMCs) treatment inhibits PDGF-stimulated vascular smooth muscle cell proliferation in a dose dependent fashion with an IC50 of 0.3 µM on day 8.
PD-161570 suppresses constitutive phosphorylation of the FGF-1 receptor in both human ovarian carcinoma cells (A121(p)) and Sf9 insect cells overexpressing the human FGF-1 receptor and blocked the growth of A121(p) cells in culture.
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis.
Cell Proliferation Assay
Cell Line:
Vascular smooth muscles cells (VSMCs)
Concentration:
0.1 µM, 0.3 µM, 1 µM
Incubation Time:
1 day, 3 days, 6 days, 8 days
Result:
Inhibited VSMC proliferation in a dose dependent fashion with an IC50 of 0.3 µM at day 8.
分子式
C26H35Cl2N7O
分子量
532.51
CAS号
192705-80-9
运输条件
Room temperature in continental US; may vary elsewhere.