1. PI3K/Akt/mTOR
    Apoptosis
    Autophagy
  2. Akt
    Apoptosis
    Autophagy
  3. TAS-117 hydrochloride

TAS-117 hydrochloride 

Cat. No.: HY-19934A
Handling Instructions

TAS-117 hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 hydrochloride induces apoptosis and autophagy.

For research use only. We do not sell to patients.

TAS-117 hydrochloride Chemical Structure

TAS-117 hydrochloride Chemical Structure

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Description

TAS-117 hydrochloride is a potent, selective, orally active allosteric Akt inhibitor (with IC50s of 4.8, 1.6, and 44 nM for Akt1, 2, and 3, respectively). TAS-117 hydrochloride triggers anti-myeloma activities and enhances fatal endoplasmic reticulum (ER) stress induced by proteasome inhibition. TAS-117 hydrochloride induces apoptosis and autophagy[1].

IC50 & Target[1]

Akt1

4.8 nM (IC50)

Akt2

1.6 nM (IC50)

Akt3

44 nM (IC50)

In Vitro

TAS-117 (1 μM; 6 hours) blocks basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt[1].
TAS-117 (0-10 μM; 72 hours) selectively inhibits Akt and induces cytotoxicity in MM cells with high baseline phosphorylation of Akt[1].
TAS-117 abrogates the cytoprotective effect of the bone marrow microenvironment associated with Akt inhibition in both MM cells and BMSCs. TAS-117 enhances Carfilzomib-induced cytotoxicity and fatal ER stress in MM cells. TAS-117 (0.5, 1 μM) triggers G0/G1 arrest followed by apoptosis, associated with induction of autophagy and endoplasmic reticulum stress response[1].
TAS-117 enhances bortezomib-induced cytotoxicity, associated with increased CHOP (a fatal ER-stress marker) and PARP cleavage and blockade of bortezomib-induced p-Akt, suggesting that TAS-117 augments Bortezomib-induced ER stress and apoptotic signaling[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay[1]

Cell Line: MM cell lines
Concentration: 0-10 μM
Incubation Time: 72 hours
Result: Induced significant growth inhibition in MM cell lines with high baseline p-Akt, but not in cell lines with low baseline p-Akt.

Western Blot Analysis[1]

Cell Line: MM.1S, MM.1R, H929, and KMS11 cells
Concentration: 1 μM
Incubation Time: 6 hours
Result: Blocked basal phosphorylation of Akt and downstream p-FKHR/FKHRL1 in MM cells with high baseline p-Akt, but did not inhibit autophosphorylation of PDK1 which phosphorylates Akt at Thr308.
In Vivo

TAS-117 (12-16 mg/kg; p.o.; daily for 5 days a week, 21 days) inhibits tumor growth in murine xenograft models of human MM[1].
TAS-117 enhances bortezomib-induced MM cytotoxicity in vivo[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SCID mice (xenograft models bearing MM.1S cells)[1]
Dosage: 12, 16 mg/kg
Administration: P.o.; daily for 5 days a week, 21 days
Result: Significantly reduced MM.1S tumor growth versus vehicle control.
Clinical Trial
Molecular Weight

460.96

Formula

C₂₆H₂₅ClN₄O₂

SMILES

C[[email protected]@](C1)(O)C[[email protected]]1(N)C2=CC=C(C3=C(N(COC4=CC=NC=C45)C5=N3)C6=CC=CC=C6)C=C2.[H]Cl

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

References
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Keywords:

TAS-117TAS117TAS 117AktApoptosisAutophagyPKBProtein kinase Ballostericoralanti-myelomaERstressproteasomeInhibitorinhibitorinhibit

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Product Name:
TAS-117 hydrochloride
Cat. No.:
HY-19934A
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