TAS-117 (Pifusertib) is a highly selective, oral, allosteric pan-AKT inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.
TAS-117 (Pifusertib) shows minimal inhibitory activities against others kinases including PI3K, PDK1, and mTOR.
TAS-117 (Pifusertib) inhibits Akt kinase activity but not p-Akt, blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1.
TAS-117 (Pifusertib) induces significant cytotoxicity in MM cells associated with inhibition of IL6 secretion.
TAS-117 (Pifusertib) triggers apoptosis and autophagy, induces ER stress response, inhibits human MM cell growth in murine xenograft models.
