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首页-小分子抑制剂&激动剂-Tyrosine Kinase-VEGFR-TAK-593
TAK-593

Chemical Structure : TAK-593

CAS No.: 1005780-62-0

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TAK-593 (TAK593)

货号: PC-25522Not For Human Use, Lab Use Only.

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

规格 价格 库存 数量
5 mg ￥1480 In stock
10 mg ￥2380 In stock
25 mg ￥3980 In stock
50 mg Get quote
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TAK-593 is a potent, selective and ATP-competitive inhibitor of tyrosine kinases VEGFR and PDGFR with IC50s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
TAK-593 strongly suppresses proliferation of VEGF-stimulated human umbilical vein endothelial cells with an IC50 of 0.30 nM。
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 exhibits strong anti-tumor effects against various human cancer xenografts.
TAK-593 shows anti-proliferative and pro-apoptotic effects on tumors along with a decrease of vessel density and inhibition of pericyte recruitment to microvessels in vivo.

物理化学性质&存储条件

分子量 445.48
分子式 C23H23N7O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

N-(5-((2-(Cyclopropanecarboxamido)imidazo[1,2-b]pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl-1H-pyrazole-5-carboxamide

参考文献

1. Iwata H, et al. Biochemistry. 2011 Feb 8;50(5):738-51.

2. Awazu Y, et al. Cancer Sci. 2013 Apr;104(4):486-94.

3. Miyamoto N, et al. Bioorg Med Chem. 2013 Apr 15;21(8):2333-2345.

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