VX-11e

Description: VX-11e is a novel, potent, selective, and orally bioavailable ERK2 (extracellular signal-related kinase 2) inhibitor with potential anticancer activity. It inhibits ERK2 with a Ki of< 2 which='' is=''> 200-fold more selective over other kinases. ERK is extracellular signal-regulated kinases, and is a key component of the Ras/Raf/MEK/ERK signal transduction pathway, which is an oncogenic pathway related to a variety of human cancers. In both rats and mice, VX-11e shows good oral bioavailability. In NSG mice bearing human melanoma RPDX tumors, VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth. When used in combination with BKM120, VX-11e results in significantly improved tumor growth inhibition.

References: J Med Chem. 2009 Oct 22; 52(20):6362-8; Clin Cancer Res. 2016 Apr 1; 22(7):1592-602.