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AT7867

In stock
Catalog No.
A5653
Akt1/2/3 and p70S6K/PKA inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$132.00
In stock
5mg
$120.00
In stock
10mg
$160.00
In stock
50mg
$680.00
In stock
100mg
$990.00
In stock

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Email: [email protected]

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Background

AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA (IC50=32 nM/17 nM/47 nM and 85 nM/20 nM, respectively).

Akt, also known as protein kinase B, is a serine/threonine-specific protein kinase that plays a key role in multiple cellular processes such as glucose metabolism, apoptosis, cell proliferation, transcription and cell migration.

AT7867 inhibited cell proliferation in multiple human cancer cell lines, it is most potent in inhibiting MES-SA uterine/MDA-MB-468/MCF-7 breast/HCT116/HT29 colon lines (IC50, 0.9–3 μM). AT7867 also inhibited GSK3β among each cell lines tested (IC50=2-4 μM). In U87MG human glioblastoma cells, AT7867 suppressed AKT signaling and induced apoptosis in a time and concentration-dependent manner. [1]

In athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model, AT7867 treatment showed inhibition in phosphorylation of AKT/p70S6K downstream substrates and led to apoptosis. In PTEN-dificient xenograft models, AT7867 inhibited human tumor growth. [1]

Reference:
Grimshaw KM, Hunter LJ, Yap TA et al.  AT7867 is a potent and oral inhibitor of AKT and p70 S6 kinase that induces pharmacodynamic changes and inhibits human tumor xenograft growth. Mol Cancer Ther. 2010 May;9(5):1100-10.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt337.85
Cas No.857531-00-1
FormulaC20H20ClN3
Solubility≥16.9mg/mL in DMSO, ≥4.38 mg/mL in EtOH with ultrasonic, ≥45 mg/mL in H2O
Chemical Name4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine
SDFDownload SDF
Canonical SMILESC1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description AT7867 is a potent ATP-competitive inhibitor of Akt1/2/3 and p70S6K/PKA with IC50 values of 32 nM/17 nM/47 nM and 85 nM/20 nM, respectively
Targets Akt2 PKA Akt1 Akt3 p70 S6K  
IC50 17 nM 20 nM 32 nM 47 nM 85 nM  

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