化学性质：                                                                                                             

产品描述：                                                                                                            

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]. Using an appropriate sarcoma lung metastasis xenograft model, NVP-BHG712 decreased lung metastasis formation (p

特别提醒：