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首页-小分子抑制剂&激动剂-PI3K/Akt/mTOR Pathway-Akt-TAS-117
TAS-117

Chemical Structure : TAS-117

CAS No.: 1402602-94-1

TAS-117 (Pifusertib, TAS117)

货号: PC-62833Not For Human Use, Lab Use Only.

TAS-117 is a highly selective, non-ATP competitive pan-Akt inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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.

物理化学性质&存储条件

分子量 424.504
分子式 C26H24N4O2
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

Trans-3-amino-1methyl-3-[4-(3-phenyl-5H-imidazo[1,2-c]pyrido[3,4-e][1,3]oxazin-2-yl)phenyl]-cyclobutanol

参考文献

1. Mimura N, et al. Cancer Res. 2014 Aug 15;74(16):4458-69.

2. Koji Ichikawa, et al. https://doi.org/10.1158/1535-7163.TARG-13-C177.

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