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

Chemical Structure : TAS-117 hydrochloride

CAS No.: 2930090-28-9

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TAS-117 hydrochloride (Pifusertib hydrochloride, TAS117)

货号: PC-63553Not For Human Use, Lab Use Only.

TAS-117 (Pifusertib) hydrochloride is a highly selective, oral, allosteric pan-AKT inhibitor with IC50 of 4.8/1.6/44 nM for Akt1/Akt2/Akt3 respectively.

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2 mg ￥2580 In stock
5 mg ￥4280 In stock
10 mg ￥7280 In stock
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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) hydrochloride 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 460.962
分子式 C26H25ClN4O2
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 hydrochloride

参考文献

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

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