TAK-593 is an effective VEGFR and PDGFR family inhibitor (IC50s: 3.2, 0.95, 1.1, 4.3, and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα, and PDFGRβ, respectively).

PDGFRβ:13 nM, VEGFR2:0.95 nM, VEGFR3:1.1 nM, VEGFR1:3.2 nM, PDGFRα:4.3 nM, PDGFRα (V561D):1 nM

TAK-593 inhibits the growth of HUVEC (IC50: 0.30 nM). TAK-593 also potently inhibits VEGF-induced tube formation of endothelial cells co-cultured with fibroblasts. 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. It displays effective 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][2].