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GSK2334470

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Catalog No. T2348Cas No. 1227911-45-6

GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.

GSK2334470

GSK2334470

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Purity: 99.87%
Catalog No. T2348Cas No. 1227911-45-6
GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
5 mg$48In StockIn Stock
10 mg$79In StockIn Stock
25 mg$148In StockIn Stock
50 mg$271-In Stock
1 mL x 10 mM (in DMSO)$87In 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:99.87%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
GSK2334470 is a novel PDK1 inhibitor (IC50: ~10 nM, in a cell-free assay), with no inhibitory at other close related AGC-kinases.
Targets&IC50
PDK1:10 nM
In vivo
The efficacy of the PDK1 inhibitor (PDKi) GSK2334470 was assessed in newborn BrafV600E::Pten?/? mice through systemic administration of 4-HT. Administering PDK1 twice weekly significantly inhibited pigmented lesions and concurrent melanomagenesis, alongside a notable reduction (~80%) in lung metastases and lymph node metastases, as quantified by H&E staining and S100 immunostaining, respectively. This outcome mirrors the effects observed with the genetic deletion of Pdk1[4].
Kinase Assay
FGFR1-4 Biochemical Assays: FGFR kinase inhibition assays are performed at KM for ATP. Picomolar to low nanomolar concentrations of FGFR proteins are incubated in 1× Kinase Reaction Buffer (KRB) with 1 μM of CSKtide and 50 to 250 of μM ATP at 25°C for 90 minutes in the presence or absence of a dosed concentration series of inhibitor. All reactions are terminated by the addition of Stop buffer, and plates are read on a Caliper EZReader2. IC50 values are fit with a four-parameter log[Inhibitor] versus response model with floating Hill Slope.
Cell Research
GSK2334470 is dissolved in DMSO and diluted with appropriate medium before use. To study the inhibitory effect of GSK2334470 on mTOR-S6K pathway, non-resistant cells and the resistant sublines are treated with GSK2334470 at 5 μM for 1.5 and 12 h in 10 % FBS medium with/without MK-2206 (5 μM)[2].
Chemical Properties
Molecular Weight462.59
FormulaC25H34N8O
Cas No.1227911-45-6
SmilesCNc1nc(cc(n1)-c1ccc2c(N)n[nH]c2c1)N1C[C@H](CC[C@H]1C)C(=O)NC1CCCCC1
Relative Density.1.30 g/cm3 (Predicted)
Storage & Solubility Information
StorageIn solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
Ethanol: 83 mg/mL (179.42 mM), Sonication is recommended.
DMSO: 150 mg/mL (324.26 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (7.13 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
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.1617 mL10.8087 mL21.6174 mL108.0871 mL
5 mM0.4323 mL2.1617 mL4.3235 mL21.6174 mL
10 mM0.2162 mL1.0809 mL2.1617 mL10.8087 mL
20 mM0.1081 mL0.5404 mL1.0809 mL5.4044 mL
50 mM0.0432 mL0.2162 mL0.4323 mL2.1617 mL
100 mM0.0216 mL0.1081 mL0.2162 mL1.0809 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

Keywords

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