1. PI3K/Akt/mTOR
    Autophagy
  2. Akt
    Autophagy
  3. CCT128930

CCT128930 

Cat. No.: HY-13260 Purity: 99.15%
Handling Instructions

CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).

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

CCT128930 Chemical Structure

CCT128930 Chemical Structure

CAS No. : 885499-61-6

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 160 In-stock
Estimated Time of Arrival: December 31
5 mg USD 145 In-stock
Estimated Time of Arrival: December 31
10 mg USD 251 In-stock
Estimated Time of Arrival: December 31
50 mg USD 818 In-stock
Estimated Time of Arrival: December 31
100 mg USD 1294 In-stock
Estimated Time of Arrival: December 31
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

Publications Citing Use of MCE CCT128930

View All Akt Isoform Specific Products:

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

Description

CCT128930 is a potent and selective inhibitor of Akt2 (IC50 6 nM) with 28-fold selectivity over the closely related PKA kinase (IC50 168 nM), as well as 20-fold selectivity over p70S6K (IC50 120 nM).

IC50 & Target[1]

Akt2

6 nM (IC50)

p70S6K

120 nM (IC50)

PKA

168 nM (IC50)

Autophagy

 

In Vitro

CCT128930 exhibits marked antiproliferative activity and inhibits the phosphorylation of a range of Akt substrates in multiple tumor cell lines in vitro, consistent with Akt inhibition. CCT128930 causes a G1 arrest in PTEN-null U87MG human glioblastoma cells, consistent with Akt pathway blockade. CCT128930 is a potent ATP-competitive Akt inhibitor, which is initially screened at 10 µM against a panel of kinases representative of the human protein kinome. In view of the potential of ATP-competitive inhibitors to cross-react with the closely related AGC class of kinases, the IC50 of CCT128930 against selected AGC kinases is determined. The GI50 values of CCT128930 for growth inhibition are 6.3 μM±2.2 (n=3) for U87MG human glioblastoma cells, 0.35 μM±0.11 (n=4) for LNCaP human prostate cancer cells, and 1.9 μM±0.80 (n=5) for PC3 human prostate cancer cells, all of which are PTEN-deficient human tumor cell lines[1].

In Vivo

The pharmacokinetics of CCT128930 after a single dose of 25 mg/kg are shown. Following i.v. administration, CCT128930 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 AUC0-∞ of 4.6 µMh. Following i.p. administration, the peak plasma drug concentration is 4-fold lower and the plasma clearance is similar to that observed i.v..The corresponding AUC0-∞ is 1.3 µMh, giving an i.p. bioavailability of 29%[1].

Molecular Weight

341.84

Formula

C₁₈H₂₀ClN₅

CAS No.

885499-61-6

SMILES

ClC1=CC=C(C=C1)CC2(CCN(CC2)C3=NC=NC4=C3C=CN4)N

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 36.67 mg/mL (107.27 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.9253 mL 14.6267 mL 29.2535 mL
5 mM 0.5851 mL 2.9253 mL 5.8507 mL
10 mM 0.2925 mL 1.4627 mL 2.9253 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (8.04 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.75 mg/mL (8.04 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.75 mg/mL (8.04 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
Kinase Assay
[1]

Profiling against 50 different human kinases is carried out using 10 μM CCT128930 at an ATP concentration equivalent to the Km for each enzyme. All other enzyme assays are performed[1].

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

Cell Assay
[1]

All cell lines are grown in their recommended culture medium, supplemented with 10% fetal bovine serum at 37°C in 5% CO2 and passaged for less than six months prior to replacement from early passage frozen stocks. CCT128930 and LY294002 are made up as 10mM stocks in DMSO. Cells are regularly screened for Mycoplasma using a PCR-based assay. Cells are seeded in 96-well plates and allowed to attach for 36 hours to ensure exponential growth prior to treatment. In vitro antiproliferative activity is determined using a 96-hour SRB assay, and GI50 values are derived[1].

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

Animal Administration
[1]

Mice[1]
PTEN-null U87MG human glioblastoma cells (2×106) are injected subcutaneously (s.c.) in the right flank of 6-8 weeks old female CrTacNCr-Fox1nu mice. For HER2-positive, PIK3CA-mutant BT474 human breast cancer xenografts, cells (5×106) are administered s.c. in medium supplemented with matrigel (1:1) into the mammary fat pads of female mice implanted s.c. with estradiol pellets (0.025 mg, 90 day release) 3 days previously. Animals are randomized and treatment is started with vehicle or CCT128930 when established tumors are ~100 mm3 in mean volume. Control mice receive vehicle only (10% DMSO, 5% Tween 20, 85% saline) and treated mice received 50 mg/kg CCT128930 intraperitoneally (i.p.) daily for 5 days (U87MG human glioblastoma xenografts) or 40 mg/kg CCT128930 i.p. twice daily for 5 days (BT474 human breast cancer xenografts). Tumor size and body weight are monitored three times a week. Tumor size is evaluated by measurement of 2 orthogonal diameters with calipers and volume is calculated. At the end of the study, tumors are excised and weighed.

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

References
  • No file chosen (Maximum size is: 1024 Kb)
  • If you have published this work, please enter the PubMed ID.
  • Your name will appear on the site.
  • Molarity Calculator

  • Dilution Calculator

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

Keywords:

CCT128930CCT 128930CCT-128930AktAutophagyPKBProtein kinase BInhibitorinhibitorinhibit

Your Recently Viewed Products:

Inquiry Online

Your information is safe with us. * Required Fields.

Product name

 

Salutation

Applicant name *

 

Email address *

Phone number *

 

Organization name *

Country or Region *

 

Requested quantity *

Remarks

Bulk Inquiry

Inquiry Information

Product name:
CCT128930
Cat. No.:
HY-13260
Quantity:
MCE Japan Authorized Agent: