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TAS-117 hydrochloride

Chemical Structure : TAS-117 hydrochloride

CAS No.: 2930090-28-9

TAS-117 hydrochloride (Pifusertib, 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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    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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