NVP-BHG712, >=98% (HPLC)

NVP-BHG712, >=98% (HPLC)

Application

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 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.

Biochem/physiol Actions

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.

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.

Features and Benefits

This compound is a featured product for Kinase Phosphatase Biology research. Click here to discover more featured Kinase Phosphatase Biology products. Learn more about bioactive small molecules for other areas of research at sigma.com/discover-bsm.

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

Packaging

5, 25 mg in glass bottle

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Code Description Colour Quality Level InChI key InChI Manufacturer Solubility Form Assay Price Quantity
3574043 NVP-BHG712, >=98% (HPLC) white to beige 100 ZCCPLJOKGAACRT-UHFFFAOYSA-N 1S/C26H20F3N7O/c1-15-8-9-16(25(37)32-19-7-3-6-18(12-19)26(27,28)29)11-21(15)33-23-20-14-31-36(2)24(20)35-22(34-23)17-5-4-10-30-13-17/h3-14H,1-2H3,(H,32,37)(H,3 SIGMA-ALDRICH DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£742.39 (exc VAT) per 25MG
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3574044 NVP-BHG712, >=98% (HPLC) white to beige 100 ZCCPLJOKGAACRT-UHFFFAOYSA-N 1S/C26H20F3N7O/c1-15-8-9-16(25(37)32-19-7-3-6-18(12-19)26(27,28)29)11-21(15)33-23-20-14-31-36(2)24(20)35-22(34-23)17-5-4-10-30-13-17/h3-14H,1-2H3,(H,32,37)(H,3 SIGMA-ALDRICH DMSO: 2 mg/mL, clear powder ≥98% (HPLC)
£185.25 (exc VAT) per 5MG
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