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AT7867 dihydrochloride

In stock
Catalog No.
A3199
Akt1 and p70S6K/PKA inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$205.00
In stock
5mg
$187.00
In stock
10mg
$250.00
In stock
50mg
$1,061.00
In stock
100mg
$1,544.00
In stock

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Email: [email protected]

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Background

IC50: AKT1 32 nM, AKT2 17 nM, AKT3 47 nM, PKA 20 nM
The serine/threonine kinase AKT plays a pivotal role in signal transduction events involved in malignant transformation and chemoresistance and is an attractive target for the development of cancer therapeutics. Structure-based drug design and fragment-based lead discovery have identified AT7867 as a novel and potent inhibitor of both AKT and the downstream kinase p70 S6 kinase (p70S6K) and also of protein kinase A.
In vitro: AT7867 potently inhibits both AKT and p70S6K activity, measured by inhibition of protein phosphorylation of GSK3β and S6 ribosomal, and also the growth inhibition in a panel of human cancer cell lines. Induction of apoptosis by AT7867 was detected by multiple methods in tumor cells followingAT7867 treatment [1].
In vivo: Administration ofAT7867 (90 mg/kg p.o. or 20 mg/kg i.p.) to athymic mice implanted with the PTEN-deficient U87MG human glioblastoma xenograft model caused inhibition of phosphorylation of downstream substrates of both AKTand p70S6K and induction of apoptosis. These AT7867 doses also led to inhibition of human tumor growth in PTEN-deficient xenograft models. These findings suggest that a novel strategy of AKT and p70S6K blockade may have therapeutic value and supports further evaluation of AT7867 as a singleagent anticancer strategy [1].
Clinical trial: Currently no clinical data are available.
References:
[1] Grimshaw KM, Hunter LJ, Yap TA, Heaton SP, Walton MI, Woodhead SJ, Fazal L, Reule M, Davies TG, Seavers LC, Lock V, Lyons JF, Thompson NT, Workman P, Garrett MD. 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;9(5):1100-10.

Chemical Properties

StorageStore at -20°C
M.Wt410.77
Cas No.1431697-86-7
FormulaC20H22Cl3N3
SynonymsAT-7867 dihydrochloride;AT 7867 dihydrochloride
SolubilitySoluble in DMSO
Chemical Name4-(4-chlorophenyl)-4-[4-(1H-pyrazol-4-yl)phenyl]piperidine;dihydrochloride
SDFDownload SDF
Canonical SMILESC1CNCCC1(C2=CC=C(C=C2)C3=CNN=C3)C4=CC=C(C=C4)Cl.Cl.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.

Quality Control

Quality Control & MSDS

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Chemical structure

AT7867 dihydrochloride