Home Protein Tyrosine Kinase Ephrin receptor inhibitor - Bcr-Abl inhibitor - Raf inhibitor - Src inhibitor NVP-BHG712 For research use only.

NVP-BHG712

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 Chemical Structure

NVP-BHG712 Chemical Structure

CAS No. 940310-85-0

Purity & Quality Control

NVP-BHG712 Related Products

Signaling Pathway

Ephrin receptor Signaling Pathways

Ephrin receptor Signaling Pathway

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]
(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
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]
Experimental Result Images Methods Biomarkers Images PMID
Western blot p-EphB4 / p-EphB2 / p-EphB3 / p-EphA2 / p-EphA3 20803239
In Vivo
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 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.

Chemical Information & Solubility

Molecular Weight 503.48 Formula

C26H20F3N7O
CAS No. 940310-85-0 SDF Download NVP-BHG712 SDF
Smiles CC1=C(C=C(C=C1)C(=O)NC2=CC=CC(=C2)C(F)(F)F)NC3=C4C=NN(C4=NC(=N3)C5=CN=CC=C5)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 101 mg/mL ( (200.6 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 3 mg/mL

Water : Insoluble


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In vivo
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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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