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AKT inhibitor VIII

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Catalog No. T3346Cas No. 612847-09-3
Alias AKTi-1/2

AKT inhibitor VIII (AKTi-1/2) is a highly specific inhibitor of Akt1/2, with IC50 values of 58 nM and 210 nM respectively, demonstrating approximately 36-fold greater selectivity for Akt1 over Akt3.

AKT inhibitor VIII

AKT inhibitor VIII

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Purity: 98.65%
Catalog No. T3346Alias AKTi-1/2Cas No. 612847-09-3
AKT inhibitor VIII (AKTi-1/2) is a highly specific inhibitor of Akt1/2, with IC50 values of 58 nM and 210 nM respectively, demonstrating approximately 36-fold greater selectivity for Akt1 over Akt3.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$61In StockIn Stock
5 mg$107In StockIn Stock
10 mg$155In StockIn Stock
25 mg$278In StockIn Stock
50 mg$397In StockIn Stock
100 mg$569In StockIn Stock
1 mL x 10 mM (in DMSO)$129In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
All TargetMol products are for research purposes only and cannot be used for human consumption. We do not provide products or services to individuals. Please comply with the intended use and do not use TargetMol products for any other purpose.
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Purity:98.65%
Color:Yellow
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Product Introduction

Bioactivity
Description
AKT inhibitor VIII (AKTi-1/2) is a highly specific inhibitor of Akt1/2, with IC50 values of 58 nM and 210 nM respectively, demonstrating approximately 36-fold greater selectivity for Akt1 over Akt3.
Targets&IC50
Akt3:2119 nM, Akt1:58 nM, Akt2:210 nM
In vitro
Akti-1/2 (50 mg/kg, i.p.) inhibits both basal and IGF-stimulated Akt1/2 phosphorylation in the lungs of mice.
In vivo
In cell-based IPKA (C33A) assays, AKT inhibitor VIII suppresses Akt1/2 with IC50 values of 305 and 2086 nM, respectively. It significantly increases caspase-3 activity, inducing apoptosis in MCF7, HT29, and A2780 cells. In hepatocytes, it inhibits insulin's regulation of PEPCK and the expression of G6Pase and FOXO1 activity. Additionally, AKT inhibitor VIII enhances PAR-1-mediated platelet aggregation by blocking PKB. It inhibits cell growth in HCC827, NCI-H522, NCI-1651, and PC-9 cells with IC50 values of 4.7, 7.25, and 9.5 μM, respectively. When combined with gefitinib, the effects of suppressing cell growth and inducing apoptosis are enhanced.
Kinase Assay
Kinase screen: Briefly, all assays (25.5 μl at 21°C for 30 min) are performed using a Biomek 2000 Laboratory Automation Workstation in a 96-well format. Reactions contains 5–20 mU purified kinase along with substrate peptide or protein and are initiated by the addition of 10 mM MgAcetate and 5, 20, or 50 μM ATP ([γ-33P]-ATP, 800 cpm/pmol).
Cell Research
The cell growth inhibitory effect of AKTi-1/2 is studied using the 96 h sulforhodamine B assay (SRB). Drug concentrations that inhibited 50% of cell growth (IC50) are calculated for each compound in GraphPad Prism 6.0 using non-linear regression analysis and sigmoidal dose–response (variable slope) equation.(Only for Reference)
SynonymsAKTi-1/2
Chemical Properties
Molecular Weight551.64
FormulaC34H29N7O
Cas No.612847-09-3
SmilesO=c1[nH]c2ccccc2n1C1CCN(Cc2ccc(cc2)-c2nc3cc4[nH]cnc4cc3nc2-c2ccccc2)CC1
Relative Density.1.351g/cm3
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 255 mg/mL (462.26 mM), Heating is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (3.63 mM), Sonication is recommended.
Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.8128 mL9.0639 mL18.1278 mL90.6388 mL
5 mM0.3626 mL1.8128 mL3.6256 mL18.1278 mL
10 mM0.1813 mL0.9064 mL1.8128 mL9.0639 mL
20 mM0.0906 mL0.4532 mL0.9064 mL4.5319 mL
50 mM0.0363 mL0.1813 mL0.3626 mL1.8128 mL
100 mM0.0181 mL0.0906 mL0.1813 mL0.9064 mL

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
TargetMol | Animal experiments For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, TargetMol | Animal experiments and a total of 10 animals are to be administered, using a formulation of TargetMol | reagent 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.
Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSOTargetMol | reagent to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSOTargetMol | reagent stock solution to 400 μL PEG300TargetMol | reagent and mix thoroughly until the solution becomes clear.

2) Add 50 μL Tween 80 and mix well until fully clarified.

3) Add 450 μL Saline,PBS or ddH2OTargetMol | reagent and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.
1 Enter information below:
mg/kg
g
μL
2 Enter the in vivo formulation:
% DMSO
%
% Tween 80
% Saline/PBS/ddH2O

Dose Conversion

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Tech Support

Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc

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