Home PI3K/Akt/mTOR Akt inhibitor - Autophagy activator - Apoptosis related activator CCT128930

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CCT128930 Akt inhibitor

Cat.No.S2635

CCT128930 is a potent, ATP-competitive and selective inhibitor of Akt2 with IC50 of 6 nM in a cell-free assay, 28-fold greater selectivity for Akt2 than the closely related PKA kinase. This compound induces cell cycle arrest, DNA damage, and autophagy independent of Akt inhibition. High dose of this chemical triggers cell apoptosis in HepG2 cells.
CCT128930 Akt inhibitor Chemical Structure

Chemical Structure

Molecular Weight: 341.84

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: S263501 DMSO]25 mg/mL]false]Ethanol]5 mg/mL]false]Water]Insoluble]false Purity: 99.18%
99.18

Cell Culture, Treatment & Working Concentration

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
U87MG cells Function assay Inhibition of PKB in human U87MG cells assessed as GSK3-beta phosphorylation by ELISA, IC50=0.66 nM
PC3M cells Function assay Inhibition of PKB in human PC3M cells assessed as GSK3-beta phosphorylation by ELISA, IC50=0.003 μM
Click to View More Cell Line Experimental Data

Chemical Information, Storage & Stability

Molecular Weight 341.84 Formula

C18H20ClN5

 Storage (From the date of receipt)
CAS No. 885499-61-6 Download SDF Storage of Stock Solutions

Synonyms N/A Smiles C1CN(CCC1(CC2=CC=C(C=C2)Cl)N)C3=NC=NC4=C3C=CN4

Solubility

In vitro
Batch:

DMSO : 25 mg/mL (73.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 5 mg/mL

Water : Insoluble

Molarity Calculator

Mass Concentration Volume Molecular Weight

In vivo
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In vivo Formulation Calculator (Clear solution)

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Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Mechanism of Action

Targets/IC50/Ki
Akt2 [1]
(Cell-free assay)
6 nM
p70 S6K [1]
(Cell-free assay)
120 nM
PKA [1]
(Cell-free assay)
168 nM
In vitro
CCT128930 exhibits marked antiproliferative activity against PTEN-deficient human tumor cell lines including U87MG human glioblastoma cells, LNCaP human prostate cancer cells and PC3 human prostate cancer cells with GI50 of 6.3 μM, 0.35 μM and 1.9 μM, respectively. Furthermore, this compound causes a G1 arrest in PTEN-null U87MG human glioblastoma cells and Akt pathway blockade. [1]
Kinase Assay
Kinase assays
Profiling against 50 different human kinases is carried out using 10 μM CCT128930 at an ATP concentration equivalent to the Km for each enzyme.
In vivo
CCT128930 at 25 mg/kg i.p. shows a marked antitumor effect in established PTEN-null U87MG human glioblastoma xenografts with a treated:control (T/C) ratio of 48% on day 12. In HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, this compound at 40 mg/kg also produces a profound antitumor effect with complete growth arrest and a T/C ratio of 29% on day 22. This chemical administrated via i.v. reaches a peak concentration of 6.4 μM in plasma and is eliminated with a relatively short half-life, high volume of distribution, and rapid clearance, giving an area under the curve AUC0-∞ of 4.6 μM h. It administrated via i.p. leads to the peak plasma drug concentration of 1.3 μM and the corresponding AUC0-∞ of 1.3 μM·h. Oral administration of this compound leads to the peak plasma concentration of only 0.43 μM and a correspondingly low AUC0-∞ of 0.4 μM·h. [1]
References

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