BAW2881 是一种选择性的VEGFR2抑制剂，其IC50=9 nM。

BAW2881 is a potent and selective VEGFR inhibitor (vascular endothelial growth factor receptor tyrosine kinase inhibitor) with activity to inhibit chronic and acute skin inflammation.

局部施用NVP-BAW2881在小鼠和家猪皮肤中,能减少VEGF-A诱导的血管通透性.NVP-BAW2881能够靶向鼠源、猪源和人源VEGFR2的酪氨酸激酶区域.NVP-BAW2881减少小鼠的皮肤损伤处白细胞浸润,减少表皮增生、正常表皮角化细胞分化以及显示较少的血管异常.NVP-BAW2881处理过的小鼠的血管变小、数量减少.相较于对照组,实验组小鼠的耳肿胀、皮肤炎症、淋巴结肿大、皮肤红斑得到改善.虽然两种给药途径都有效（口服和局部施用）,但全身性用药比局部给药更为强效.

体外实验证明NVP-BAW2881能够抑制人淋巴管内皮细胞和脐静脉内皮细胞的增殖、迁移以及小管生成。

HUVECs or LECs (1.2×103) were seeded into fibronectin-coated 96-well plates. After 24 hours, the cells were transferred into LEC medium containing 2% fetal bovine serum and incubated for an additional 24 hours. Cells(eight wells/condition) were incubated with medium alone(control), 20 ng/ml VEGF-A, or a combination of 20 ng/ml VEGF-A and 1 nmol/L to 1 mol/L NVP-BAW2881. Proliferation was also assayed in LECs incubated with 500 ng/ml VEGF-C. The dimethyl sulfoxide concentration was adjusted to 0.1% in all wells. After 72 hours, cells were incubated with 5-methylumbelliferylheptanoate for subsequent fluorescent quantification of viable cells, using a SpectraMax Gemini electron microscope. (Only for Reference)

861875-60-7

C22H15F3N4O2

424.383

BAW2881

H2O:<1 mgml
DMSO:78 mg/mL (183.8 mM)
Ethanol:16 mg/mL (37.7 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years