Name: NVP-BHG712
Price: 292.00 USD

- Overview
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    Background
    
    NVP-BHG712 is a potent inhibitor of EphB4 and VEGFR2 with ED50 value of 25 nM and 4200 nM, respectively [1].
    Ephrin type-B receptor 4 (EphB4) is a protein and plays an important role in mediating a variety of developmental processes by working with its ligand. It has been revealed that the over-expression of EphB4 is correlated with several types of tumor [1, 3].
    NVP-BHG712 is a potent EphB4 inhibitor and has less inhibition activity on EphB2, EphA2, EphB3 and EphA3. When tested with Hek293 cells transfected different EphRs, administration of NVP-BHG712 inhibited EphRs autophosphorylation in a dose-dependent manner with preference for EphB4, followed by EphB2, EphA2, EphB3 and EphA3 [1]. In HEK293/ABCC 10 cell line, NVP-BHG712 treatment markedly increased cells sensitivity to paclitaxel at the dose of 0.25 μM and 0.5μM [2]. When treated synovial sarcoma cell line with NVP-BHG712, the result showed that it markedly decreased cell proliferation rate and vitality [3].
    In VEGF driven angiogenesis tissue model, NVP-BHG712 treatment significantly inhibited VEGF stimulated tissue formation and vascularization by functioning on EphB4 which involved in VEGF driven angiogenesis [1]. In HEK293/ABCC 10 cells subcutaneous xenograft mouse model, co-administration of NVP-BHG712 (25 mg/kg) and paclitaxel (15 mg/kg) markedly decreased tumor volumes, sizes and weights [2].
    
    [1]. Martiny-Baron, G., et al., The small molecule specific EphB4 kinase inhibitor NVP-BHG712 inhibits VEGF driven angiogenesis. Angiogenesis, 2010. 13(3): p. 259-67.
    [2]. Kathawala, R.J., et al., The small molecule tyrosine kinase inhibitor NVP-BHG712 antagonizes ABCC10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study. Oncotarget, 2015. 6(1): p. 510-21.
    [3]. Becerikli, M., et al., EPHB4 tyrosine-kinase receptor expression and biological significance in soft tissue sarcoma. Int J Cancer, 2015. 136(8): p. 1781-91.
- Properties
  - Alternative Name
    
    4-methyl-3-[(1-methyl-6-pyridin-3-ylpyrazolo[3,4-d]pyrimidin-4-yl)amino]-N-[3-(trifluoromethyl)phenyl]benzamide
    
    CAS Number
    
    940310-85-0
    
    Molecular Formula
    
    C26H20F3N7O
    
    Molecular Weight
    
    503.48
    
    Appearance
    
    A solid
    
    Purity
    
    98.00%
    
    Solubility
    
    ≥25.15 mg/mL in DMSO; insoluble in H2O; ≥6.69 mg/mL in EtOH with ultrasonic
    
    Storage
    
    Store at -20°C
    
    * For Research Use Only
- Reference
  - 1. Tiancheng Li, Han Wang, et al. "The role of EphB4/ephrinB2 signaling in root repair after orthodontically-induced root resorption." Am J Orthod Dentofacial Orthop. 2021 Mar;159(3):e217-e232. PMID:33487501
    2. Tiancheng Li, Han Wang, et al. "Intermittent parathyroid hormone promotes cementogenesis via ephrinB2‐EPHB4 forward signaling." J Cell Physiol. 2020 Aug 1. PMID:32740946

NVP-BHG712

NVP-BHG712

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