1. Protein Tyrosine Kinase/RTK
  2. Ephrin Receptor

NVP-BHG712 

Cat. No.: HY-13258
Handling Instructions

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.

For research use only. We do not sell to patients.
NVP-BHG712 Chemical Structure

NVP-BHG712 Chemical Structure

CAS No. : 940310-85-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO $92 In-stock
5 mg $83 In-stock
10 mg $165 In-stock
50 mg $820 In-stock
100 mg $1400 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

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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. IC50 value: 25 nM(EC50) Target: EphB4 receptor;c-Raf; c-Src in vitro: NVP-BHG712 treatment also dose dependently leads to the inhibition of RTK autophosphorylation in stable transfected A375 melanoma cells with EC50 of 25 nM and 4.2 μM for EphB4 and VEGFR2, respectively [1]. in vivo: In a growth factor-induced angiogenesis model, NVP-BHG712 (3 mg/kg, p.o) significantly suppresses VEGF stimulated tissue formation and vascularization by inhibiting EphB4 forward signaling. Furthermore, NVP-BHG712 (10 mg/kg/kg, p.o.) potently reverses VEGF enhanced tissue formation and vessel growth. NVP-BHG712 (3 mg/kg, p.o.) shows a long lasting exposure with concentrations around 10 μM in plasma as well as in lung and liver tissue for up to 8 hours, and thus results in a long lasting inhibition of EphB4 kinase activity in mice [1].

References
Preparing Stock Solutions
Concentration Volume (DMSO) Mass 1 mg 5 mg 10 mg
1 mM 1.9862 mL 9.9309 mL 19.8618 mL
5 mM 0.3972 mL 1.9862 mL 3.9724 mL
10 mM 0.1986 mL 0.9931 mL 1.9862 mL
References
Molecular Weight

503.48

Formula

C₂₆H₂₀F₃N₇O

CAS No.

940310-85-0

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

10 mM in DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
NVP-BHG712
Cat. No.:
HY-13258
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