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NVP-BAW2881

CAS No. : 861875-60-7

MCE 国际站：NVP-BAW2881

产品活性：NVP-BAW2881 (BAW2881) 是有效，选择性的 VEGFR2 抑制剂，IC₅₀ 为值9 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Tie  |  VEGFR

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. 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 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.

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