同义名 :	-
	CAS号 :	1005780-62-0
	货号 :	A929254
	分子式 :	C23H23N7O3
	纯度 :	99%+
	分子量 :	445.47
	MDL号 :	MFCD23160045
	存储条件：	Pure form Sealed in dry, 2-8°C In solvent -20°C:3-6个月-80°C:12个月
	溶解度 :	-
	动物实验配方：

生物活性

描述

TAK-593 inhibits growth of HUVEC with an IC50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC50=3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC50=4.3, 13 nM) families. Against other kinases, the IC50 values of TAK-593 are above 100 nM, except for Fms (IC50=10 nM) and Ret (IC50=18 nM) kinases[1]. TAK-593 robustly suppresses VEGF- and PDGF-driven cellular phosphorylation and proliferation in human umbilical vein endothelial cells as well as human coronary artery smooth muscle cells. Additionally, it effectively halts VEGF-induced endothelial cell tube formation in co-cultures with fibroblasts[2].

实验方案
	1mg	5mg	10mg
1 mM 5 mM 10 mM	2.24mL 0.45mL 0.22mL	11.22mL 2.24mL 1.12mL	22.45mL 4.49mL 2.24mL

参考文献

[1]Miyamoto N, et al. Discovery of N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,2-b]pyridazin-6-yl}oxy)-2-methylphenyl]-1,3-dimethyl-1H-pyrazole-5-carboxamide (TAK-593), a highly potent VEGFR2 kinase inhibitor. Bioorg Med Chem. 2013 Apr 15;21(8):2333-2345. [2]Awazu Y, et al. Anti-angiogenic and anti-tumor effects of TAK-593, a potent and selective inhibitor of vascular endothelial growth factor and platelet-derived growth factor receptor tyrosine kinase. Cancer Sci. 2013 Apr;104(4):486-94.