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。
| 生物活性 | PD-089828 is an ATP competitive inhibitor ofFGFR-1,PDGFR-βandEGFR(IC50s=0.15, 1.76, and 5.47 μM, respectively) and a noncompetitive inhibitor ofc-Srctyrosine kinase (IC50=0.18 μM). PD-089828 also inhibitsMAPKwith anIC50of 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]. |
| IC50& Target[1] | FGFR1 0.15 μM (IC50) | PDGFR-β 1.76 μM (IC50) | EGFR 5.47 μM (IC50) | c-Src 0.18 μM (IC50) | FGFR1 0.14 μM (Ki) | PDGFR-β 2.38 μM (Ki) | EGFR 3.16 μM (Ki) | c-Src 0.1 μM (Ki) |
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体外研究
(In Vitro) | PD-089828 (0.5-20 μM; 2 hours) inhibits PDGFR autophosphorylation with an IC50of 0.82 μM[1].
PD-089828 (1-50 μM; 2 hours) inhibits EGFR autophosphorylation with an IC50value of 10.9 μM[1].
In A121(p) cells, PD 089828 potently inhibits the phosphorylation of FGFR-1 with an IC50value of 0.63 μM[1].
PD-089828 (10 μM; 8 days) produces a concentration-related inhibition of serum-stimulated cell growth with an IC50value of 1.8 μM[1].
PD-089828 inhibits increases in DNA synthesis stimulated by all three growth factors, with IC50values of 0.8 for PDGF-, 1.7 for EGF- and 0.48 μM for bFGF-induced mitogenesis[1].
Cell Proliferation Assay[1] | 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[1] | 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 IC50of 0.82 μM. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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