Name: NVP-BHG712
Brand: SIGMA

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About This Item

经验公式（希尔记法）:

C₂₆H₂₀F₃N₇O

CAS Number:

940310-85-0

分子量:

503.48

MDL编号:

MFCD20272929

UNSPSC代码:

12352200

PubChem化学物质编号:

329825338

NACRES:

NA.77

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质量水平

100

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

−20°C

SMILES字符串

Cc1ccc(cc1Nc2nc(nc3n(C)ncc23)-c4cccnc4)C(=O)Nc5cccc(c5)C(F)(F)F

InChI

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,33,34,35)

InChI key

ZCCPLJOKGAACRT-UHFFFAOYSA-N

应用

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.

生化/生理作用

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.

特点和优势

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.