BAW2881

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

BAW2881 是一种有效的选择性 VEGFR 抑制剂（血管内皮生长因子受体酪氨酸激酶抑制剂），具有抑制慢性和急性皮肤炎症的活性。

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. NVP-BAW2881 inhibited proliferation, migration, and tube formation by human umbilical vein endothelial cells and lymphatic endothelial cells in vitro. NVP-BAW2881 reduced the number of blood and lymphatic vessels and infiltrating leukocytes in the skin, and normalized the epidermal architecture. NVP-BAW2881 also displayed strong anti-inflammatory effects in models of acute inflammation; pretreatment with topical NVP-BAW2881 significantly inhibited VEGF-A-induced vascular permeability in the skin of pigs and mice.

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. 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.

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.

BAW2881 | BAW-2881 | BAW 2881

Others

Other Targets

c-Abl| B-Raf (V599E)| C-Raf-1| hVEGFR2

Endocrinology

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861875-60-7

424.38

C22H15F3N4O2

>98% (HPLC)

DMSO : ≥ 33 mg/mL; 77.76 mM

O=C(c1c2ccc(Oc3nc(N)ncc3)cc2ccc1)Nc1cccc(C(F)(F)F)c1

6-((2-aminopyrimidin-4-yl)oxy)-N-(3-(trifluoromethyl)phenyl)-1-naphthamide

(-20℃)

With Ice Pack

≥ 2 years