For research use only.

Catalog No.S2202

8 publications

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.

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Selleck's NVP-BHG712 has been cited by 8 publications

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Choose Selective Ephrin receptor Inhibitors

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.
EphB4 [1]
(cell based assays )
C-Raf [1]
(Cell-free assay)
c-Src [1]
(Cell-free assay)
c-Abl [1]
(Cell-free assay)
25 nM(ED50) 0.395 μM 1.266 μM 1.667 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]

Methods Test Index PMID
Western blot
p-EphB4 / p-EphB2 / p-EphB3 / p-EphA2 / p-EphA3 ; 

PubMed: 20803239     

NVP-BHG712 inhibits multiple Eph receptor kinases in cell based assays. Different EphR full length cDNAs have been transiently expressed in Hek293 cells. EphR autophosphorylation has been initiated by stimulating cells for 30 min with either 1 μg/ml ephrinA1-Fc (EphA2, EphA3) or a combination of 1 μg/ml ephrinB1-Fc and 1 μg/ml ephrinB2-Fc. NVPBHG712 was added 1 h prior cell stimulation and autophosphorylation was monitored by immuno-precipitation of EphR protein followed by western analysis using anti-phospho-tyrosine antibodies.

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]


Animal Research:[1]
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  • Animal Models: VEGF-mediated angiogenesis in vivo is induced in a growth factor implant model in mice.
  • 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 Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
NMP+PEG300 (10+90, v+v)
For best results, use promptly after mixing.
30 mg/mL

* 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


CAS No. 940310-85-0
Storage powder
in solvent
Synonyms N/A
Smiles C[N]1N=CC2=C1N=C(N=C2NC3=CC(=CC=C3C)C(=O)NC4=CC=CC(=C4)C(F)(F)F)C5=CC=CN=C5

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Ephrin receptor Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID