NVP-BHG712

NVP-BHG712 has been used as an ephrin type-B receptor 4 (Eph-B4) inhibitor to study its effect on Eph-B4 phosphorylation in ephrin-B2/Fc stimulated mouse lung endothelial cells.

NVP-BHG712 has been used as an epinephrine type-B receptor 4 (Eph-B4) inhibitor:

• to study its effects on human colorectal cancer cell growth in vitro and the growth of tumor cells in mice.
• to study the regulation of endothelial nitric oxide synthase.
• to study its effects on vascularization and growth of endometriotic lesions.

NVP-BHG712 (4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide) inhibits the activity of ABC transporter subfamily C member 10 (ABCC10), which is responsible for mediating paclitaxel resistance. Therefore, NVP-BHG712 in combination with paclitaxel is effective against cancers that are resistant to paclitaxel due to the expression of the ABCC10.

NVP-BHG712 is a potent, selective EphB4 kinase inhibitor.

NVP-BHG712 is a very potent, selective inhbitor of the receptor tyrosine kinase EphB4 (ED₅₀ = 25 nM). NVP-BHG712 blocks Ephrin receptor autophosphorylation and VEGF-induced angiogenesis.

NVP-BHG712 obstructs angiogenesis mediated by vascular endothelial growth factor in vivo. It also blocks the efflux of ATP-binding cassette (ABC) transporter subfamily C member 10 (ABCC10) into the HEK293 cells by overexpressing the ABCC10 transporter.

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This compound is featured on the Eph page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.