TAK-593 (C007B-585642)

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 VitroTAK-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 VivoTAK-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:SolidIC50& 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 )

Specifictaions: Moligand™, ≥98%

MDL Number: C23H23N7O3

Molecular Formula: 445.47

PubChem CID: 24767976

Isomeric SMILES: CC1=C(C=C(C=C1)OC2=NN3C=C(N=C3C=C2)NC(=O)C4CC4)NC(=O)C5=CC(=NN5C)C