S87796 |
JK-P3 |
| 源叶(MedMol) | 98% |
- 产品描述： JK-P3 is a potent and pan VEGFR2 inhibitor, with IC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well as fibroblast growth factor receptor kinase activity in vitro. JK-P3 has anti-angiogenic activity
- 靶点： VEGFR2:7.83 μM (IC50);FGFR1:27 μM (IC50);FGFR3:5.18 μM (IC50)
- 体外研究：
JK-P3 (0.01-10 μM; 1 hour) inhibits VEGF-A-mediated VEGFR2 phosphorylation and downstream signalling. JK-P3 (0.01-10 μM; 16 hours) dose not inhibit HUVEC cell proliferation at 0.01~1 μM, and shows slight inhibitory activity at 10 μM. JK-P3 (1 and 10 μM; 1 hour) does not significantly inhibit VEGF-A-stimulated endothelial tube formation at 1 µM, but almost completely inhibits the ability of endothelial cells to form into elongated hollow tubes in the presence of VEGF-A at 10 µM. Western Blot Analysis Cell Line: Primary endothelial cells (treated for 7.5 min with 25 ng/mL VEGF-A) Concentration: 0.01, 0.1, 1 and 10 μM Incubation Time: 1 hour Result: Almost completely inhibited VEGFR2 Y1175 phosphorylation, also inhibited VEGF-A-stimulated PLCγ1, Akt and ERK1/2 phosphorylation. Cell Proliferation Assay Cell Line: HUVEC Concentration: 0.01, 0.1, 1 and 10 μM Incubation Time: 16 hours Result: Failed to inhibit endothelial cell proliferation at 0.01~1 μM but elicited a small but significant increase in cell proliferation at certain lower concentrations.
- 参考文献：
1. Kankanala J, et al. A combinatorial in silico and cellular approach to identify a new class of compounds that target VEGFR2 receptor tyrosine kinase activity and angiogenesis. Br J Pharmacol. 2012;166(2):737-748.
- 溶解性： Soluble in DMSO
- 保存条件： 2-8℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 3.093 ml 15.463 ml 30.926 ml 5 mM 0.619 ml 3.093 ml 6.185 ml 10 mM 0.309 ml 1.546 ml 3.093 ml 50 mM 0.062 ml 0.309 ml 0.619 ml
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。
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