货号	规格	价格	上海	北京	珠海	重庆	武汉
S81625-1mg促销	≥98%	￥170.00 ￥152.00 S81625-1mg ￥152.00 现货	4 0 4	-	-	-	-
S81625-5mg促销	≥98%	￥590.00 ￥530.00 S81625-5mg ￥530.00 现货	4 4	-	-	-	-
S81625-25mg促销	≥98%	￥2110.00 ￥1890.00 S81625-25mg ￥1890.00 现货	2 2	-	-	-	-
S81625-100mg促销	≥98%	￥4360.00 ￥3920.00 S81625-100mg ￥3920.00 现货	1 1	-	-	-	-

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产品描述：

TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.

靶点：

VEGFR1:3.2 nM (IC50);VEGFR2:0.95 nM (IC50);VEGFR3:1.1 nM (IC50);PDGFRα:4.3 nM (IC50);PDGFRβ:13 nM (IC50);PDGFRαV561D:1 nM (IC50);VEGFR; PDGFR

体外研究：

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. TAK-593 potently inhibits VEGF- and PDGF-stimulated cellular phosphorylation and proliferation of human umbilical vein endothelial cells and human coronary artery smooth muscle cells. TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts

体内研究：

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.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.245 ml	11.224 ml	22.448 ml
5 mM	0.449 ml	2.245 ml	4.49 ml
10 mM	0.224 ml	1.122 ml	2.245 ml
50 mM	0.045 ml	0.224 ml	0.449 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。

参考文献

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