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PF-AKT400 (Synonyms: AKT protein kinase inhibitor)

Catalog No. T5508 Copy Product Info
Purity: 98.21%
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PF-AKT400 (AKT protein kinase inhibitor) is a broadly selective and ATP-competitive inhibitor of Akt.

PF-AKT400

Copy Product Info
🥰Excellent
Catalog No. T5508
Synonyms AKT protein kinase inhibitor

PF-AKT400 (AKT protein kinase inhibitor) is a broadly selective and ATP-competitive inhibitor of Akt.

PF-AKT400
Cas No. 1004990-28-6
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Pack SizePriceUSA StockGlobal StockQuantity
1 mg$96In Stock-
5 mg$239In Stock-
10 mg$343In Stock-
25 mg$579In Stock-
50 mg$829In Stock-
100 mg$1,150InquiryInquiry
1 mL x 10 mM (in DMSO)$263In Stock-
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Purity:98.21%
Appearance:Solid
Color:White
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Product Introduction

PF-AKT400 AI Summary
PF-AKT400 shows potent bioactivity based on multiple assays. It exhibits high oral bioavailability in various animal models, such as dogs and rats, and excellent inhibitory activity against AKT1 and AKT2 in IMAP assays, with IC50 values of 0.5 nM and 9.0 nM, respectively. The compound demonstrates selectivity towards AKT1 over other kinases like RSK3, RSK2, PKG1alpha, MSK2, MSK1, and CDK7. Additionally, it shows antitumor activity against human PC3 and COLO205 cells xenografted in SCID/Beige mice, resulting in significant tumor growth inhibition. PF-AKT400 effectively inhibits the AKT1/p70S6K1 signaling pathways, leading to reduced phosphorylation levels of S6 protein, and exhibits strong AKT1/p70S6K1 inhibition in both single-dose and multiple-dose administrations, as well as feedback loop-associated activities. These data suggest that PF-AKT400 has promising potential as a candidate for further development as an anticancer therapy targeting the AKT signaling pathway..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
PF-AKT400 (AKT protein kinase inhibitor) is a broadly selective and ATP-competitive inhibitor of Akt.
Targets&IC50
PKBα:0.5 nM, PKA:450 nM
SynonymsAKT protein kinase inhibitor
Chemical Properties
Molecular Weight400.43
FormulaC20H22F2N6O
Cas No.1004990-28-6
SmilesCCc1c[nH]c2ncnc(N3CC[C@](N)(CNC(=O)c4ccc(F)cc4F)C3)c12
Relative Density.1.353 g/cm3
Storage & Solubility Information
StorageShipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 90 mg/mL (224.76 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (8.24 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 mM2.4973 mL12.4866 mL24.9732 mL124.8658 mL
5 mM0.4995 mL2.4973 mL4.9946 mL24.9732 mL
10 mM0.2497 mL1.2487 mL2.4973 mL12.4866 mL
20 mM0.1249 mL0.6243 mL1.2487 mL6.2433 mL
50 mM0.0499 mL0.2497 mL0.4995 mL2.4973 mL
100 mM0.0250 mL0.1249 mL0.2497 mL1.2487 mL
Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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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

You can also refer to dose conversion for different animals. More Dose Conversion

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

Keywords

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