PD 089828 是 FGFR-1、PDGFR-β 和 EGFR 的 ATP 竞争性抑制剂（IC50s\u003d0.15、1.76 和 5.47 μM）和 c-Src 酪氨酸激酶的非竞争性抑制剂（IC50\u003d0.18 μM）。 PD 089828 还抑制 MAPK，IC50 为 7.1 μM。 PD 089828 在体外抑制 PDGF、EGF 和 bFGF 介导的酪氨酸激酶受体自磷酸化。 PD 089828 具有持久的细胞活性。
| Cas No. | 179343-17-0 |
| Canonical SMILES | NC(N=C1)=NC(C1=C2)=NC(NC(NC(C)(C)C)=O)=C2C3=C(Cl)C=CC=C3Cl |
| 分子式 | C18H18Cl2N6O |
| 分子量 | 405.3 |
| 溶解度 | DMSO: 25 mg/ml,Ethanol: 1 mg/ml |
| 储存条件 | Store at -20°C |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request |
| 产品描述 | PD 089828 is a competitive inhibitor of the receptor tyrosine kinases FGFR1, PDGFRβ, and EGFR (IC50s = 0.15, 1.76, and 5.47 µM, respectively) and a noncompetitive inhibitor of the nonreceptor tyrosine kinase c-Src (IC50 = 0.18 µM). It is selective for these targets over insulin receptor tyrosine kinase, PKC, and CDK4 (IC50s = >50 µM) but does inhibit MAPK (IC50 = 7.1 µM). PD 089828 decreases PDGF-BB-, EGF-, and bFGF-induced phosphorylation of PDGFR, EGFR, and FGFR1, respectively, in a concentration-dependent manner in vitro. It also decreases serum-stimulated growth (IC50 = 1.8 µM after 8 days) and migration (IC50 = 4.5 µM) of rat aortic smooth muscle cells. |
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