940310-85-0

Basic information

• Product Name: NVP-BHG712
• Synonyms: NVP-BHG712;4-Methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide;4-methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluoromethyl)phenyl)benzamide;NVP-BHG712 4-Methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]benzamide;4-Methyl-3-(1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidin-4-ylamino)-N-(3-(trifluorome
• CAS NO: 940310-85-0
• Molecular Formula: C26H20F3N7O
• Molecular Weight: 503.49
• Product Categories: Inhibitors
• Mol File: 940310-85-0.mol

Chemical Properties

• Appearance: white to beige/
• Density: 1.41
• Storage Temp.: ?20°C
• Solubility: DMSO: >15mg/mL
• PKA: 13.20±0.70(Predicted)
• CAS DataBase Reference: NVP-BHG712(CAS DataBase Reference)
• NIST Chemistry Reference: NVP-BHG712(940310-85-0)
• EPA Substance Registry System: NVP-BHG712(940310-85-0)

Safety Data

• Hazard Codes: T
• Statements: 25
• Safety Statements: 45
• RIDADR: UN 2811 6.1 / PGIII
• WGK Germany: 3
• Hazardous Substances Data: 940310-85-0(Hazardous Substances Data)

Usage

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.

references

[1]. martiny-baron, g., et al., the small molecule specific ephb4 kinase inhibitor nvp-bhg712 inhibits vegf driven angiogenesis. angiogenesis, 2010. 13(3): p. 259-67.[2]. kathawala, r.j., et al., the small molecule tyrosine kinase inhibitor nvp-bhg712 antagonizes abcc10-mediated paclitaxel resistance: a preclinical and pharmacokinetic study. oncotarget, 2015. 6(1): p. 510-21.[3]. becerikli, m., et al., ephb4 tyrosine-kinase receptor expression and biological significance in soft tissue sarcoma. int j cancer, 2015. 136(8): p. 1781-91.

Upstream product

• 91092-05-6 1-methyl-6-(pyridin-3-yl)-1H-pyrazolo[3,4-d]pyrimidine-4-amine 
• 7697-26-9 3-bromo-4-methylbenzoic acid 
• 21900-33-4 3-bromo-4-methylbenzoyl chloride 
• 98-16-8 3-trifluoromethylaniline 
• 856860-16-7 5-amino-1-methyl-1H-pyrazole-4-carbonitrile 

Relevant articles and documents

SUBSTITUTED PENTA-FUSED HEXA-HETEROCYCLIC COMPOUNDS, PREPARATION METHOD THEREFOR, DRUG COMBINATION AND USE THEREOF

A type of substituted penta-fused hexa-heterocyclic compounds having selective inhibition for PIKfyve kinase, a pharmaceutically acceptable salt and pharmaceutically acceptable solvate thereof, a method for the preparation thereof, a pharmaceutical composition comprising the same, and use of these compounds in the manufacture of a medicament for preventing or treating a disease associated with PIKfyve in vivo, in particular in the manufacture of a medicament for preventing or treating tumor growth and metastasis.

NVP-BHG712: Effects of Regioisomers on the Affinity and Selectivity toward the EPHrin Family

Erythropoietin-producing hepatocellular (EPH) receptors are transmembrane receptor tyrosine kinases. Their extracellular domains bind specifically to ephrin A/B ligands, and this binding modulates intracellular kinase activity. EPHs are key players in bid

3-(SUBSTITUTED AMINO)-PYRAZOLO[3,4-d]PYRIMIDINES AS EPHB AND VEGFR2 KINASE INHIBITORS

The invention relates to novel pyrazolo[3,4-d]pyrimidines of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their use as medicaments and to medicaments comprising them.