A selective

NVP-BHG712 – 25 mg

Brand:
Cayman
CAS:
940310-85-0
Storage:
-20
UN-No:
De Minimis - 2811 / 6.1

The EphB4 receptor tyrosine kinase (cloned from erythropoietin-producing hepatocellular carcinoma) and its ligand ephrinB2 play an important role in embryonic vessel development and vascular remodeling. Signaling from this pair is also involved in tumor angiogenesis. NVP-BHG712 is an orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 = 25 nM).{29822} It is selective for EphB4, demonstrating an ED50 value of 4.2 µM at the related VEGFR2 receptor and ED50 values >10 µM against a panel of 40 additional kinases.{29822} At 3-30 mg/kg, NVP-BHG712 dose dependently inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis.{29822}  

 

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Description

A selective, orally bioavailable inhibitor of EphB4 kinase autophosphorylation (ED50 =25 nM); inhibits VEGF-directed vessel formation in an in vivo mouse model of angiogenesis

Formal name: 4-methyl-3-[[1-methyl-6-(3-pyridinyl)-1H-pyrazolo[3,4-d]pyrimidin-4-yl]amino]-N-[3-(trifluoromethyl)phenyl]-benzamide

Synonyms: 

Molecular weight: 503.5

CAS: 940310-85-0

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Other Receptor Tyrosine Kinases||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Angiogenesis||Research Area|Cancer|Cell Signaling||Research Area|Cell Biology|Cell Signaling|Growth Factor Receptors

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