TAK-593 is a potent VEGFR and PDGFR family inhibitor with IC 50 s of 3.2, 0.95, 1.1, 4.3 and 13 nM for VEGFR1, VEGFR2, VEGFR3, PDFGRα and PDFGRβ, respectively.
In Vitro
TAK-593 inhibits growth of HUVEC with an IC 50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC 50 =3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC 50 =4.3, 13 nM) families. Against other kinases, the IC 50 values of TAK-593 are above 100 nM, except for Fms (IC 50 =10 nM) and Ret (IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
TAK-593 inhibits growth of HUVEC with an IC 50 of 0.30 nM. It shows potent inhibitory activity against VEGFR (VEGFR1-3: IC 50 =3.2, 0.95, 1.1 nM) and PDGFR (PDGFRα, β: IC 50 =4.3, 13 nM) families. Against other kinases, the IC 50 values of TAK-593 are above 100 nM, except for Fms (IC 50 =10 nM) and Ret (IC 50 =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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
