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

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

Alix Tröster, Stephanie Heinzlmeir, Benedict-Tilman Berger, Santosh L Gande, Krishna Saxena, Sridhar Sreeramulu, Verena Linhard, Amir H Nasiri, Michael Bolte, Susanne Müller, Bernhard Kuster, Guillaume Médard, etc.

ChemMedChem. 2018 Aug 20;13(16):1629-1633.

PMID: 29928781

Abstract:

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 bidirectional intercellular signaling, controlling cell morphology, adhesion, and migration. They are increasingly recognized as cancer drug targets. We analyzed the binding of NVP-BHG712 (NVP) to EPHA2 and EPHB4. Unexpectedly, all tested commercially available NVP samples turned out to be a regioisomer (NVPiso) of the inhibitor, initially described in a Novartis patent application. They only differ by the localization of a single methyl group on either one of two adjacent nitrogen atoms. The two compounds of identical mass revealed different binding modes. Furthermore, both in vitro and in vivo experiments showed that the isomers differ in their kinase affinity and selectivity.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP940310850	NVP-BHG712		940310-85-0	Price

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