JK-P3

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Chemical Structure| 942655-44-9 同义名 : -
CAS号 : 942655-44-9
货号 : A709575
分子式 : C18H17N3O3
纯度 : 99%+
分子量 : 323.346
MDL号 : MFCD22666405
存储条件：

Pure form Inert atmosphere,2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(154.63 mM)，配合低频超声，并水浴加热至45℃助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
描述 JK-P3 is a potent pan-VEGFR2 inhibitor with IC50 values of 7.83 μM, 27 μM and 5.18 μM for VEGFR2, FGFR1 and FGFR3, respectively. JK-P3 inhibits VEGF-A-stimulated VEGFR2 activation and intracellular signalling, and endothelial monolayer wound closure and angiogenesis. JK-P3 inhibited VEGF-A-stimulated VEGFR2 activation and intracellular signaling, as well as endothelial monolayer closure and angiogenesis, and also inhibited fibroblast growth factor receptor kinase activity in vitro. JK-P3 possesses anti-angiogenic activity. JK-P3 inhibits VEGF-A-mediated VEGFR2 phosphorylation and downstream signalling at concentrations of 0.01-10 μM for 1 h. At concentrations less than 1 μM, JK-P3 inhibits VEGFR2 phosphorylation and downstream signalling. At doses less than 1 μM for 16 h, JK-P3 did not inhibit HUVEC cell proliferation. At a dose of 10 µM, JK-P3 showed slight inhibitory activity. At a concentration of 1 µM, JK-P3 did not significantly inhibit VEGF-A-stimulated endothelial cell tube formation, but at a concentration of 10 µM, JK-P3 almost completely inhibited VEGF-A-stimulated endothelial cells to form into elongated hollow tubes [1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.09mL

0.62mL

0.31mL

15.46mL

3.09mL

1.55mL

30.93mL

6.19mL

3.09mL
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.