BAW 2881 is a vascular endothelial growth factor receptor (VEGFR) inhibitor (IC50s = 0.82, 0.037, and 0.42 μM for hVEGFR1, 2, and 3, respectively). It inhibits Tie2 and RET with IC50 values of 0.65 and 0.41 μM, respectively, but demonstrates IC50 values > 10 μM toward a large panel of additional kinases. BAW 2881 was shown to block VEGF-A-induced proliferation, migration, and tube formation of human umbilical vein endothelial cells and lymphatic endothelial cells in vitro. In a mouse model of psoriasis, both oral and topical administration of BAW 2881 reduced psoriasis-like inflammation in ear skin. Topical application of BAW 2881 also reduced VEGF-A-induced vascular permeability and inhibited contact hypersensitivity reactions and UV-B-induced erythema in the skin of domestic pigs.
