179343-17-0 PD089828

• 生物活性 PD-089828 是 ATP 竞争性 FGFR-1、PDGFR-β 和 EGFR (IC50 分别为 0.15, 1.76, 5.47 µM) 抑制剂和 c-Src 酪氨酸激酶非竞争性抑制剂 (IC50=0.18 µM)。PD-089828 也抑制 MAPK，IC50 值为 7.1 µM。PD-089828 体外抑制 PDGF-、EGF- 和 bFGF 介导的酪氨酸激酶受体的自磷酸化。PD-089828 具有持久的细胞活性。
• 靶点 FGFR1 0.15 μM (IC 50 ) PDGFR-β 1.76 μM (IC 50 ) EGFR 5.47 μM (IC 50 ) c-Src 0.18 μM (IC 50 ) FGFR1 0.14 μM (Ki) PDGFR-β 2.38 μM (Ki) EGFR 3.16 μM (Ki) c-Src 0.1 μM (Ki)
• 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.

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