TAK-593

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. IC50 & Target: IC50: 3.2 nM (VEGFR1), 0.95 nM (VEGFR2), 1.1 nM (VEGFR3), 4.3 nM (PDFGRα), 13 nM (PDFGRβ)^[1] 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^[1]. 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^[2]. 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^[1]. 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^[2].