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TAK-593

CAS No. : 1005780-62-0

MCE 国际站：TAK-593

产品活性：TAK-593是有效的 VEGFR2 和 PDGFR 抑制剂，对VEGFR1, VEGFR2, VEGFR3, PDFGRα 和 PDFGRβ 的 IC₅₀ 值分别为3.2，0.95，1.1，4.3 和 13 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：PDGFR  |  VEGFR

In Vitro: 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.

In Vivo: 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.

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