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AG1024

🥰Excellent
Catalog No. T2693Cas No. 65678-07-1
Alias Tyrphostin AG 1024, AGS 200

AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).

AG1024

AG1024

🥰Excellent
Purity: 99.37%
Catalog No. T2693Alias Tyrphostin AG 1024, AGS 200Cas No. 65678-07-1
AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
2 mg$34In StockIn Stock
5 mg$52In StockIn Stock
10 mg$88In StockIn Stock
25 mg$163In StockIn Stock
50 mg$247In StockIn Stock
100 mg$372In StockIn Stock
1 mL x 10 mM (in DMSO)$58In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
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Purity:99.37%
Color:White to Yellow
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Product Introduction

Bioactivity
Description
AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).
Targets&IC50
IGF-1R:7 μM, Insulin receptor:57 μM
In vitro
In mice carrying Ba/F3-p210 xenografts, the administration of AG-1024 (30 μg) for 10 days significantly inhibited tumor growth.
In vivo
AG-1024 effectively inhibits autophosphorylation of the IGF-1 receptor (IC50=7 μM) and IR (IC50=57 μM). In MCF-7 cells, at a concentration of 10 μM, AG-1024 downregulates phosphorylated Akt1 and bcl-2, while upregulating Bax, p53, and p21, thereby inhibiting cell proliferation.
Kinase Assay
Inhibition of IGF-1- and insulin-stimulated cellular proliferation: NIH-3T3 cells overexpressing IGF-1 or insulin receptors are plated on 96-well plates (2,000-5,000 cells/well) and maintained overnight in complete medium. Cells are then changed to DMEM containing 1% FBS in the presence of 10 nM IGF-1 or insulin and various concentrations of AG-1024 for 120 hours. Medium is replaced every 48 hours. At the indicated periods of time, the medium is aspirated from the wells and 100 μL MTT is added to each well. The cells are then incubated for 4 hours at 37 °C and lysed by addition of 100 μL isoamylic alcohol and shaking for 20 minutes. The plate is then read in the ELISA reader at 570 and 690 nm. The IC50 value is calculated at the 120-hour time point.
Cell Research
Cells are exposed to AG-1024 for 24, 48 or 72 hours. For the determination of proliferation, cells are harvested and counted with trypan blue dye exclusion. Apoptosis is evaluated by dual staining of MCF-7 with fluoresceine anti-digoxigenin and propidium iodide. Briefly, fixed cells are washed with PBS, suspended in TdT buffer with TdT enzyme and Dig-dUTP for 60 minutes, and suspended in FITC blocking solution with anti-Dig-Fluorescein for 30 minutes at room temperature and kept in a dark place. Cells are then rinsed in buffer and resuspended in propidium iodide/RNase A solution for 30 minutes then analyzed by flow cytometry. For the assessment of phospho-Akt1, Bax, p53, bcl-2 and p21, cells are lysed and analyzed by western blot.(Only for Reference)
SynonymsTyrphostin AG 1024, AGS 200
Chemical Properties
Molecular Weight305.17
FormulaC14H13BrN2O
Cas No.65678-07-1
SmilesCC(C)(C)c1cc(C=C(C#N)C#N)cc(Br)c1O
Relative Density.1.42g/cm3
Storage & Solubility Information
Storagestore at low temperature,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 75 mg/mL (245.76 mM), Sonication is recommended.
Ethanol: < 1 mg/mL (insoluble or slightly soluble)
H2O: < 1 mg/mL (insoluble or slightly soluble)
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 2 mg/mL (6.55 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 mM3.2769 mL16.3843 mL32.7686 mL163.8431 mL
5 mM0.6554 mL3.2769 mL6.5537 mL32.7686 mL
10 mM0.3277 mL1.6384 mL3.2769 mL16.3843 mL
20 mM0.1638 mL0.8192 mL1.6384 mL8.1922 mL
50 mM0.0655 mL0.3277 mL0.6554 mL3.2769 mL
100 mM0.0328 mL0.1638 mL0.3277 mL1.6384 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

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

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