General description
一种有效的VEGFR酪氨酸激酶抑制剂。
BAW2881 (NVP-BAW2881) is a VEGFR inhibitor.Vascular endothelial growth factor (VEGF) is a potent endothelial cell mitogen regulating blood and lymphatic vessel development and homeostasis. There are three main subtypes of VEGFR, numbered VEGFR 1, 2 and 3.
In vitro: Previous study showed that BAW2881 could inhibit a limited number of kinases including c-RAF, B-RAF, RET, ABL, and TIE-2 at submicromole IC50s. BAW2881 could also inhibit the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases. Moreover, low IC50 value (0.12 ± 0.06 nM) demonstrated that BAW2881 remarkably abrogated VEGF induced proliferation
In vivo: In a psoriasis mouse model, BAW2881 was able to reduce the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalize the epidermal architecture. BAW2881 also showed strong anti-inflammatory effects in acute inflammation models. Moreover, the pretreatment with topical BAW2881 could significantly inhibit VEGF-A-induced vascular permeability in the skin of both pigs and mice. In addition, it was found that the topical application of BAW2881 was able to reduce the inflammatory response in pig skin caused by UV-B irradiation or by contact hypersensitivity reactions .
BAW2881（NVP-BAW2881）是一种VEGFR抑制剂。血管内皮生长因子（VEGF）是一种有效的内皮细胞促有丝分裂剂，可调节血液和淋巴管的发育及体内平衡。 VEGFR有三种主要亚型，编号为VEGFR 1、2和3。
体外：先前的研究表明，BAW2881可以在亚微摩尔IC50处抑制有限数量的激酶，包括c-RAF，B-RAF，RET，ABL和TIE-2。 BAW2881还可以抑制配体诱导的RET，PDGFR和KIT激酶的自磷酸化。此外，低的IC50值（0.12±0.06 nM）证明BAW2881显着消除了VEGF诱导的增殖
体内：在牛皮癣小鼠模型中，BAW2881能够减少血液和淋巴管的数量以及皮肤中浸润的白细胞的数量，并使表皮结构正常化。在急性炎症模型中，BAW2881还显示出强大的抗炎作用。而且，用局部BAW2881进行的预处理可以显着抑制VEGF-A诱导的猪和小鼠皮肤中的血管通透性。另外，发现BAW2881的局部施用能够减少由UV-B辐射或接触性超敏反应引起的猪皮肤中的炎症反应。
Properties
| Iupac Name： | 6-((2-aminopyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide |
| Inchi Code | 1S/C22H15F3N4O2/c23-22(24,25)14-4-2-5-15(12-14)28-20(30)18-6-1-3-13-11-16(7-8-17(13)18)31-19-9-10-27-21(26)29-19/h1-12H,(H,28,30)(H2,26,27,29) |
| Inchi Key | MLLQJNIKDWEEFT-UHFFFAOYSA-N |
安全信息
