ENMD-2076 Tartrate is a multi-targeted kinase inhibitor with IC50s of 1.86, 14, 58.2, 15.9, 92.7, 70.8, 56.4 nM for Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, PDGFRα, respectively. It is for research use only and not sold to patients.
- Acts as a multi-targeted kinase inhibitor
- Inhibits Aurora A, Flt3, KDR/VEGFR2, Flt4/VEGFR3, FGFR1, FGFR2, Src, and PDGFRα
- Shows selective inhibition of Aurora A over Aurora B
- Inhibits human umbilical vein endothelial cell (HUVEC) growth
- Blocks cellular Flt3 ligand (FL)-induced Flt3 autophosphorylation
- Prevents stem cell factor (SCF)-induced Kit autophosphorylation
- Inhibits VEGFR2/KDR autophosphorylation
- Demonstrates dose-dependent inhibition of tumor growth or tumor regression in vivo
- Exhibits good tolerance in daily doses during in vivo studies