tas-117

TAS-117, a PKB Akt inhibitor, is used potentially for the treatment of solid tumors.

TAS-117 hydrochloride 是一种选择性的、有效的、口服具有活力的别构 Akt 抑制剂，作用于 Akt1 (IC50: 4.8 nM) 、Akt2 (IC50: 1.6 nM) 和 Akt3 (IC50: 44 nM)。TAS-117 hydrochloride 能够激发抗骨髓瘤活性，增强蛋白酶体抑制诱导的致命内质网应激，可以诱导细胞凋亡和自噬。