eFT508 is a potent inhibitor of MAPK interacting protein kinases (MNK) 1 and 2 (IC50s = <10 nM). It inhibits phosphorylation of eukaryotic initiation factor 4E (eIF4E) with an IC50 value of <50 nM in a cellular signaling assay. eFT508 has a half-life of 5.3 hours in rats.
6''-[(6-Amino-4-pyrimidinyl)amino]-8''-methylspiro[cyclohexane-1,3''(2''H)-imidazo[1,5-a]pyridine]-1'',5''-dione was used in the study of inhibitors of immune checkpoint modulators and related methods. eFT508 is a potent, highly selective, and orally bioavailable MNK1 and MNK2 inhibitor.
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