tcsc0995 VX-11e

VX-11e is a potent, selective, and orally bioavailable inhibitor of ERK with K_i < 2 nM.

In Vitro: VX-11e is active in the HT29 cell proliferation assay (IC₅₀=48 nM)^[1].

In Vivo: VX-11e is orally bioavailable in both rat and mice^[1]. VX-11e (50 mg/kg, p.o.) results in robust inhibition of pRSK, and inhibits tumor growth in NSG mice bearing human melanoma RPDX tumors. VX-11e with BKM120 significantly improves tumor growth inhibition^[2].