JK-P3

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

JK-P3 

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。

JK-P3

JK-P3 Chemical Structure

CAS No. : 942655-44-9

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生物活性

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[1].

IC50 & Target[1]

VEGFR2

7.83 μM (IC50)

FGFR1

27 μM (IC50)

FGFR3

5.18 μM (IC50)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

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.

分子量

323.35

Formula

C18H17N3O3

CAS 号

942655-44-9

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.

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.

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