JK-P3 是一种有效且具有广谱性的VEGFR2抑制剂，对 VEGFR2、FGFR1 和 FGFR3 的IC50分别为 7.83 μM、27 μM 和 5.18 μM。JK-P3 可以抑制 VEGF-A 刺激的 VEGFR2 激活和细胞内信号转导，也可以抑制内皮单层细胞迁移和血管生成，以及成纤维细胞生长因子受体激酶在体外的活性。JK-P3 具有抗血管生成的活性。
| 生物活性 | JK-P3 is a potent and panVEGFR2inhibitor, withIC50s of 7.83 μM, 27 μM and 5.18 μM for VEGFR2,FGFR1andFGFR3, respectively. JK-P3 can inhibit VEGF-A-stimulated VEGFR2 activation and intracellular signalling, also inhibits endothelial monolayer wound closure and angiogenesis, as well asfibroblast growth factorreceptor kinase activityin vitro. JK-P3 has anti-angiogenic activity[1]. |
| IC50& Target[1] | VEGFR2 7.83 μM (IC50) | FGFR1 27 μM (IC50) | FGFR3 5.18 μM (IC50) |
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体外研究
(In Vitro) | JK-P3 (0.01-10 μM; 1 hour) inhibits VEGF-A-mediated VEGFR2 phosphorylation and downstream signalling[1].
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[1].
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[1].
Western Blot Analysis | Cell Line: | Primary endothelial cells (treated for 7.5 min with 25 ng/mL VEGF-A)[1] | | 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[1] | | 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. |
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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. |
