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CCT128930

In stock
Catalog No.
A8617
AKT inhibitor
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$133.00
In stock
5mg
$120.00
In stock
10mg
$210.00
In stock
50mg
$680.00
In stock
100mg
$1,020.00
In stock

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Email: [email protected]

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Background

CCT128930 is a potent, selective, novel and ATP-competitive inhibitor for AKT2 (IC50= 6 nM). It also has 28-fold and 20-fold selectivity over PKA kinase (IC50= 168 nM) and p70S6K (IC50= 120 nM), respectively.

Akt (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.

In multi tumor cell line, CCT128930 showed antiproliferative effect and blocked the phosphorylation of various Akt substrates. In PTEN-null human glioblastoma cells (U87MG), CCT128930 treatment led to a G1 arrest associated with Akt pathway suppression. [1]

In U87MG tumor xenografts, CCT128930 inhibited the phosphorylation of Akt downstream biomarkers. In U87MG, HER-2 positive and IK3CA-mutant BT474 human breast cancer xenografts, antitumor activity were recorded as tumor volume decreased. CCT128930-treated mouse whisker folliciles in vivo and human hair follicles treated ex vivo exerted prominent reduction in pThr246 PRAS40. [1]

Reference:
1. Yap TA, Walton MI, Hunter LJ et al.  Preclinical pharmacology, antitumor activity, and development of pharmacodynamic markers for the novel, potent AKT inhibitor CCT128930. Mol Cancer Ther. 2011 Feb;10(2):360-71.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt341.84
Cas No.885499-61-6
FormulaC18H20ClN5
Solubility≥17.1mg/mL in DMSO
Chemical Name4-[(4-chlorophenyl)methyl]-1-(7H-pyrrolo[2,3-d]pyrimidin-4-yl)piperidin-4-amine
SDFDownload SDF
Canonical SMILESC1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4
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 CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM.
Targets Akt2 p70 S6K PKA      
IC50 6 nM 120 nM 168 nM      

Quality Control

Quality Control & MSDS

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Chemical structure

CCT128930