Briciclib is a water soluble derivative of ON 013100, and has the potential in targeting eIF4E for solid cancers.
Briciclib has the potential in targeting eIF4E. Briciclib shows inhibitory activity against the proliferation of mantle cell leukemia (EKO-1 and MINO), breast (MCF7 and MDA-MB-231), gastric (AGS), and esophageal (OE19, OE33, and FLO-1) cancer cell lines with GI50s of 9.8-12.2 nM, and with no toxicity on normal endothelial cells. Briciclib dose-dependently reduces the expression of cyclin D1 and c-Myc in breast and MCL cancer cell lines within 8 hours[1].
References:
[1]. Neel Jasani, et al. Abstract 1649: Potent anticancer activity of an orally bioavailable small molecule, ON 013100, and its water soluble derivative, briciclib, a clinical-stage eIF4E-targeted agent. Cancer Research. August 2015, Volume 75, Issue 15.