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TAS-117 hydrochloride

Chemical Structure : TAS-117 hydrochloride

CAS No.: 2930090-28-9

TAS-117 hydrochloride (Pifusertib hydrochloride, TAS117)

Catalog No.: 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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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

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.

Physicochemical Properties

M.Wt 460.962
Formula C26H25ClN4O2
Appearance Solid
CAS No.
Storage
Solide Powder
-20 °C 12 Months; 4°C 6 Months
In Solvent
-80 °C 6 Months; -20°C 6 Months
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

References

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

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