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NVP-BHG712

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Catalog No. T6348Cas No. 940310-85-0

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.

NVP-BHG712

NVP-BHG712

🥰Excellent
Purity: 97.96%
Catalog No. T6348Cas No. 940310-85-0
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 SizePriceAvailabilityQuantity
1 mg$31In Stock
2 mg$44In Stock
5 mg$72In Stock
10 mg$113In Stock
25 mg$223In Stock
50 mg$413In Stock
100 mg$618In Stock
1 mL x 10 mM (in DMSO)$80In Stock
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Purity:97.96%
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Product Introduction

Bioactivity
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
EphB4:25 nM, C-Raf:0.395 μM, c-Src:1.266 μM, 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.
Chemical Properties
Molecular Weight503.48
FormulaC26H20F3N7O
Cas No.940310-85-0
SmilesCc1ccc(cc1Nc1nc(nc2n(C)ncc12)-c1cccnc1)C(=O)Nc1cccc(c1)C(F)(F)F
Relative Density.1.41 g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 24.7 mg/mL (40 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9862 mL9.9309 mL19.8618 mL99.3088 mL
5 mM0.3972 mL1.9862 mL3.9724 mL19.8618 mL
10 mM0.1986 mL0.9931 mL1.9862 mL9.9309 mL
20 mM0.0993 mL0.4965 mL0.9931 mL4.9654 mL

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