Powder: -20°C for 3 years | In solvent: -80°C for 1 year
NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
Pack Size | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 31.00 | |
2 mg | In stock | $ 44.00 | |
5 mg | In stock | $ 72.00 | |
10 mg | In stock | $ 113.00 | |
25 mg | In stock | $ 223.00 | |
50 mg | In stock | $ 413.00 | |
100 mg | In stock | $ 618.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 80.00 |
Description | NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively. |
Targets&IC50 | c-Src:1.266 μM, C-Raf:0.395 μM, EphB4:25 nM, c-ABL:1.667 μM |
In vitro | In a vascularization model induced by growth factors, NVP-BHG712 (3 mg/kg, p.o) significantly inhibited tissue formation and vascularization stimulated by VEGF through the suppression of EphB4 forward signaling. Additionally, NVP-BHG712 (10 mg/kg, oral administration) effectively reversed the VEGF-enhanced tissue formation and angiogenesis. NVP-BHG712 (3 mg/kg, orally) exhibited a sustained exposure in mouse plasma as well as lung and liver tissues for up to 8 hours at approximately 10 μM concentration, thereby resulting in long-lasting inhibition of EphB4 kinase activity. |
In vivo | NVP-BHG712 exhibits dose-dependent inhibition of RTK autophosphorylation in A375 melanoma cells stably transfected, with EC50 values of 25 nM for EphB4 and 4.2 μM for VEGFR2. |
Molecular Weight | 503.48 |
Formula | C26H20F3N7O |
CAS No. | 940310-85-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 24.7 mg/mL(40 mM)
You can also refer to dose conversion for different animals. More
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