NVP-BAW2881

NVP-BAW2881 (BAW2881) is a potent and selective VEGFR2 inhibitor with an IC₅₀ of 9 nM^[1][2]. IC50 & Target:IC50: 9 nM (VEGFR2)^[1] In Vitro:The VEGF-driven cellular receptor autophosphorylation in CHO cells of BAW2881 is inhibited with an IC₅₀ of 4 nM. BAW2881 inhibits a limited number of kinases including c-RAF, B-RAF, RET, ABL, and TIE-2 at sub-μM IC₅₀s^[1].
NVP-BAW2881 is highly selective for VEGFR, although it also demonstrates activity against Tie2 (IC₅₀=650 nM) and RET (IC₅₀=410 nM). The IC₅₀ values of NVP-BAW2881 toward a wide panel of other kinases are >10 μM. NVP-BAW2881 inhibits VEGF-A-induced phosphorylation of VEGFR-2 in HUVECs and in VEGFR-2-transfected Chinese hamster ovary cells, with IC₅₀ values of 2.9 and 4.2 nM, respectively^[2]. In Vivo:In a transgenic mouse model of psoriasis, NVP-BAW2881 reduces the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalized the epidermal architecture. NVP-BAW2881 also displays strong anti-inflammatory effects in models of acute inflammation; pretreatment with topical NVP-BAW2881 significantly inhibits VEGF-A-induced vascular permeability in the skin of pigs and mice^[2].