SML0333
NVP-BHG712
≥98% (HPLC)
别名:
4-Methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]-benzamide
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关于此项目
经验公式（希尔记法）:
C26H20F3N7O
化学文摘社编号:
分子量:
503.48
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
产品名称
NVP-BHG712, ≥98% (HPLC)
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)
SMILES string
Cc1ccc(cc1Nc2nc(nc3n(C)ncc23)-c4cccnc4)C(=O)Nc5cccc(c5)C(F)(F)F
InChI key
ZCCPLJOKGAACRT-UHFFFAOYSA-N
assay
≥98% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
−20°C
Quality Level
相关类别
Application
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.
Biochem/physiol Actions
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.
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.
signalword
Danger
hcodes
Hazard Classifications
Acute Tox. 3 Oral
存储类别
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Eph-B4 mediates vein graft adaptation by regulation of endothelial nitric oxide synthase
Wang M, et al.
Journal of Vascular Surgery, 65(1), 179-189 (2017)
Yujia Wang et al.
The Journal of biological chemistry, 290(22), 14235-14244 (2015-04-24)
EPH kinases are the largest family of receptor tyrosine kinases, and their ligands, ephrins (EFNs), are also cell surface molecules. This work presents evidence that EPHB4 on vascular smooth muscle cells (VSMCs) is involved in blood pressure regulation. We generated
Christin Neuber et al.
Molecules (Basel, Switzerland), 25(21) (2020-11-07)
In a previous study, EphB4 was demonstrated to be a positive regulator of A375-melanoma growth but a negative regulator of tumor vascularization and perfusion. To distinguish between EphB4 forward and ephrinB2 reverse signaling, we used the commercially available EphB4 kinase
Mo Wang et al.
Journal of vascular surgery, 65(1), 179-189 (2016-01-29)
Vein graft adaptation is characterized by loss of expression of the tyrosine kinase receptor Eph-B4, the embryonic determinant of venous identity, without increased expression of its ligand ephrin-B2, the embryonic determinant of arterial identity. Endothelial nitric oxide synthase (eNOS) is
Jeannette Rudzitis-Auth et al.
British journal of pharmacology, 177(14), 3225-3239 (2020-03-08)
The development of endometriotic lesions is crucially dependent on the formation of new blood vessels. In the present study, we analysed whether this process is regulated by erythropoietin-producing hepatoma receptor B4 (EphB4) signalling. We first assessed the anti-angiogenic action of
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