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TAS-117 hydrochloride

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产品名称: TAS-117 hydrochloride
产品型号: GOY-Y2839
产品展商: 谷研
产品文档: 无相关文档
发布时间:2023-05-04

简单介绍

TAS-117 hydrochlorideDMSO : 62.5 mg/mL (135.59 mM; ultrasonic and warming and heat to 60°C)


TAS-117 hydrochloride  的详细介绍

性能参数

产品名称

TAS-117 hydrochloride

规格

5 mg 10 mg 25 mg

货号

GOY-Y2839

 含量

>98.00%

CAS

N/A

别名

N/A

 

 

化学名

N/A

分子式

C26H25ClN4O2

分子量

分子量 460.96

溶解度

DMSO : 62.5 mg/mL (135.59 mM; ultrasonic and warming and heat to 60°C)

储存条件

Store at -20°C

General tips

 

用途

仅供科研

价格

电询

详细内容

TAS-117 hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 hydrochloride induces apoptosis and autophagy[1].

TAS-117 (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt[1].TAS-117 (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt[1].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[1].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[1].

 

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