TAK-593 是一种 VEGFR2 和 PDGFR 抑制剂，能够作用于VEGFR1 (IC50:3.2 nM)、VEGFR2 (IC50:0.95 nM)、VEGFR3 (IC50:1.1 nM)、PDFGRα (IC50:4.3 nM)、PDFGRβ (IC50:13 nM)。

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).

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].

1005780-62-0

C23H23N7O3

445.47

DMSO:45 mg/mL (101.02 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years