PD-161570 是一种有效的且具有 ATP 竞争能力的人FGF-1受体抑制剂，IC50为 39.9 nM，Ki为 42 nM。PD-161570 还抑制PDGFR，EGFR和c-Src酪氨酸激酶，IC50值分别为 310 nM，240 nM 和 44 nM。PD-161570 抑制PDGF刺激的自磷酸化和FGF-1受体磷酸化，IC50分别为 450 nM 和 622 nM。PD-161570 还是一种骨形态发生蛋白 (BMPs) 和TGF-β信号抑制剂。
| 生物活性 | PD-161570 is a potent and ATP-competitivehumanFGF-1receptorinhibitor with anIC50of 39.9 nM and aKiof 42 nM. PD-161570 also inhibits thePDGFR,EGFRandc-Src tyrosine kinaseswithIC50values of 310 nM, 240 nM, and 44 nM, respectively. PD-161570 inhibitsPDGF-stimulated autophosphorylation andFGF-1receptorphosphorylation withIC50s of 450 nM and 622 nM, respectively[1][2]. PD-161570 is also abone morphogenetic proteins (BMPs)andTGF-β signalinginhibitor[3]. |
| IC50& Target[1][2][3] | FGFR1 39.9 nM (IC50) | FGFR1 42 nM (Ki) | FGFR1 autophosphorylation 622 nM (IC50) | PDGFRβ 262 nM (IC50) | PDGFR 310 nM (IC50) | EGFR 240 nM (IC50) | c-Src 44 nM (IC50) | TGF-β Receptor |
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体外研究
(In Vitro) | 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 IC50of 0.3 μM on day 8[1].
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[2].
PD-161570 can potently inhibit basic fibroblast growth factor (bFGF)-mediated angiogenesis[4].
Cell Proliferation Assay[1] | 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 IC50of 0.3 μM at day 8. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | | Powder | -20°C | 3 years | | 4°C | 2 years | | In solvent | -80°C | 6 months | | -20°C | 1 month |
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| 溶解性数据 | In Vitro: DMSO : 33.33 mg/mL(62.59 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.8779 mL | 9.3895 mL | 18.7790 mL | | 5 mM | 0.3756 mL | 1.8779 mL | 3.7558 mL | | 10 mM | 0.1878 mL | 0.9389 mL | 1.8779 mL |
*请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 |
