eIF4A3-IN-1q

A potent, subtype-selective, orally available eIF4A3 inhibitor with IC50 of 0.14 uM; displays no activity against eIF4A1, eIF4A2, BRR2 and DHX29 (IC50>100 uM); upregulates SC35 1.6 kb mRNA expression by 8-fold at 3 uM and 20-fold at 10 uM, potently inhibit cell growth in HCT-116 cells (GI50=1.18 uM) ; shows antitumor efficacy and promising PK profiles in vivo, without severe body weight loss.

References 1. Mizojiri R, et al. ACS Med Chem Lett. 2017 Sep 8;8(10):1077-1082. View Related Products by Target Eukaryotic Initiation Factor (eIF)