NVP-BHG712

Catalog No.S2202

NVP-BHG712 Chemical Structure

Molecular Weight(MW): 503.48

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.

Size Price Stock Quantity  
In DMSO USD 340 In stock
USD 170 In stock
USD 320 In stock
USD 970 In stock

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Purity & Quality Control

Choose Selective Ephrin receptor Inhibitors

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

Biological Activity

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.
Features Discriminates between VEGFR and EphB4.
Targets
EphB4 [1] C-Raf [1] c-Src [1] c-Abl [1] Tie-2 [1]
25 nM(ED50) 0.395 μM 1.266 μM 1.667 μM >10 μM
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]

Protocol

Animal Research
+ Expand
  • Animal Models: VEGF-mediated angiogenesis in vivo is induced in a growth factor implant model in mice.
  • Formulation: NVP-BHG712 is dissolved in 1-Methyl-2-pyrrolidone (NMP) and then diluted with polyethylene glycol 300 (PEG300) to a final concentration of 10% v/v NMP and 90% v/v PEG300.
  • Dosages: ≤30 mg/kg
  • Administration: Administered via p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 101 mg/mL (200.6 mM)
Ethanol 3 mg/mL (5.95 mM)
Water <1 mg/mL
In vivo NMP+polyethylene glycol 300 (10+90, v+v) 30 mg/mL

* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 503.48
Formula

C26H20F3N7O

CAS No. 940310-85-0
Storage powder
in solvent
Synonyms N/A

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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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Ephrin receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID