TAK-593

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. Form:Solid IC50& Target:VEGFR1 3.2 nM (IC 50 ) VEGFR2 0.95 nM (IC 50 ) VEGFR3 1.1 nM (IC 50 ) PDGFRα 4.3 nM (IC 50 ) PDGFRβ 13 nM (IC 50 ) PDGFRα V561D 1 nM (IC 50 )

No numbering system information yet

No physical and chemical property information yet

No safety information yet

No production method and use information yet

No upstream information yet

No downstream information yet

No related product information yet