Chemical Structure : TAS-117
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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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.
分子量 | 424.504 | |
分子式 | C26H24N4O2 | |
外观性状 | Solid | |
储存条件 |
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Solubility |
10 mM in DMSO |
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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