BAW2881

SKU: orb1223025

Description

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.

Key Properties

• CAS Number: 861875-60-7
• MW: 424.38
• Purity: >98% (HPLC)
• Formula: C₂₂H₁₅F₃N₄O₂
• SMILES: O=C(c1c2ccc(Oc3nc(N)ncc3)cc2ccc1)Nc1cccc(C(F)(F)F)c1
• Target: c-Abl| B-Raf (V599E)| C-Raf-1| hVEGFR2
• Solubility: DMSO : ≥ 33 mg/mL; 77.76 mM

Bioactivity

• 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.
• 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.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BAW2881 | BAW-2881 | BAW 2881

Quick Database Links

Gene Symbol

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