AMG-Tie2-1 is an inhibitor of tunica interna endothelial cell kinase 2 (Tie2) and VEGF receptor 2 (VEGFR2) with IC50 values of 1 and 3 nM, respectively, in a homogenous time-resolved fluorescence (HTRF) assay.1 It inhibits angiopoietin 1-induced Tie2 autophosphorylation in EA.hy926 human endothelial cells (IC50 = 10 nM).
|1. Hodous, B.L., Geuns-Meyer, S.D., Hughes, P.E., et al. Evolution of a highly selective and potent 2-(pyridin-2-yl)-1,3,5-triazine Tie-2 kinase inhibitor. J. Med. Chem. 50(4), 611-626 (2007).