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S81625

TAK-593

源叶(MedMol) 98%
  • 英文名:
  • TAK-593
  • 别名:
  • TAK 593; UNII-H3I42X8XX7; 1H-Pyrazole-5-carboxamide,N-(5-((2-((cyclopropylcarbonyl)amino)imidazo(1,2-b)pyridazin-6-yl)oxy)-2-methylphenyl)-1,3-dimethyl; N-[5-({2-[(cyclopropylcarbonyl)amino]imidazo[1,
  • CAS号:
  • 1005780-62-0
  • 分子式:
  • C23H23N7O3
  • 分子量:
  • 445.4738
品牌货号产品规格价格(RMB) 库存(上海) 北京 武汉 南京 数量计量单位 加入购物车...
源叶(MedMol) S81625-5mg 98% ¥1860.00元 预计交期:2-3天 - - - EA 加入购物车
源叶(MedMol) S81625-10mg 98% ¥2750.00元 预计交期:2-3天 - - - EA 加入购物车
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  • 提示:详情请下载说明书。
  • 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:
    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
  • 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
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