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TAS-117 hydrochloride

CAS No. :

MCE 站：TAS-117 hydrochloride

产品活性：TAS-117 hydrochloride 是一种有效、选择性、具有口服活性的别构 Akt 抑制剂 (对 Akt1、2 和 3 的 IC₅₀ 分别为 4.8、1.6 和 44 nM)。TAS-117 hydrochloride 激发抗骨髓瘤活性并增强蛋白酶体抑制诱导的致命内质网应激。TAS-117 hydrochloride 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。

研究领域：PI3K/Akt/mTOR  |  Apoptosis  |  Autophagy

作用靶点：Akt  |  Apoptosis  |  Autophagy

In Vitro: TAS-117 (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt.
TAS-117 (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt.
TAS-117 abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. TAS-117 enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. TAS-117 (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response.
TAS-117 enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that TAS-117 augments Bortezomib-induced ER stress and apoptotic signaling.

In Vivo: TAS-117 (12-16 mg/kg; p.o.; daily for 5 days a week, 21 days) inhibits tumor growth in murine xenograft models of human MM.
TAS-117 enhances bortezomib-induced MM cytotoxicity in vivo.

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