BAW2881 (NVP-BAW2881)

BAW2881 (NVP-BAW2881)是一种新型的VEGFR酪氨酸激酶抑制剂。在1.0-4.3 nM浓度下能有效地抑制VEGFR1-3；在45-72 nM的浓度下，抑制PDGFRβ, c-Kit和RET (c-RET)。

Information

BAW2881 (NVP-BAW2881) is a novelvascular endothelial growth factor (VEGF) receptor tyrosine-kinaseinhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET (c-RET) at 45-72 nM concentrations.

Targets

hVEGFR2 (Cell-free assay); C-Raf-1 (Cell-free assay); B-RAFV599E (Cell-free assay); c-Abl (Cell-free assay); mVEGF2 (Cell-free assay) 16390,9 nM; 24 nM; 76 nM; 99 nM; 165 nM

In vitro

In vitro studies demonstrated that NVP-BAW2881 inhibited proliferation, migration, and tube formation of human umbilical vein endothelial cells and lymphatic endothelial cells.

In vivo

NVP-BAW2881 targets the tyrosine kinase domain of murine, porcine, and human VEGFR2. It can be administered both orally and topically, but has not been tested in humans. In vivo studies in VEGF-A transgenic mice showed that oral and topical administration of NVP-BAW2881 strongly reduced psoriasis-like inflammation in ear skin. Histologically, skin lesions in treated mice showed reduced infiltration by leukocytes, reduced epidermal hyperproliferation, normalization of epidermal keratinocyte differentiation, and fewer vascular abnormalities. Vessels in treated mice were smaller in size and fewer in number. In comparison to control mice, treated mice showed significant improvement in ear swelling, skin inflammation, lymph node enlargement, and skin erythema. Though both modes of administration were effective, systemic administration of NVP-BAW2881 was more potent than topical administration. Topical NVP-BAW2881 also effectively reduced VEGF-A-induced vascular permeability in the skin of mice and domestic pigs.

Cell Research(from reference)

Cell lines：Human dermal lymphatic endothelial cells(LECs), human umbilical vein endothelial cells(HUVECs) 

Concentrations：1 nmol/L to 1 mol/L 

Incubation Time：72 h