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AGI-43192

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Catalog No. T9729Cas No. 2377491-54-6

AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.

AGI-43192

AGI-43192

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Purity: 99.89%
Catalog No. T9729Cas No. 2377491-54-6
AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.
Pack SizePriceUSA WarehouseGlobal WarehouseQuantity
1 mg$69In StockIn Stock
5 mg$173In StockIn Stock
10 mg$277In StockIn Stock
25 mg$457In StockIn Stock
50 mg$642In StockIn Stock
100 mg$858In StockIn Stock
500 mg$1,730-In Stock
1 mL x 10 mM (in DMSO)$190In StockIn Stock
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In Stock Estimated shipping dateUSA Warehouse[1-2 days] Global Warehouse[5-7 days]
This molecule is a custom-made product. TargetMol has an excellent synthesis team with the experience and capability to provide you with cost-effective products.If you have any questions, please feel free to contact us. We are committed to serving you wholeheartedly.
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:99.89%
Appearance:Solid
Color:Orange
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Product Introduction

AGI-43192 AI Summary
AGI-43192 is a bioactive compound exhibiting potent inhibition of MAT2A in MTAP-null human HCT-116 cells, with an IC50 of 14.0 nM and an Imax of 80.0%. It is involved in the transactivation of human PXR and induces CYP450 expression. The compound has good cell membrane permeability and an efflux ratio of 1.8. In mouse models, it has low brain penetration (brain-to-plasma ratio < 0.1) and is primarily hepatically cleared (extraction ratio of 0.245). It has a moderate volume of distribution at steady state (Vdss = 1.98 L.kg-1) and a mean residence time of 8.1 hours. The compound demonstrates high Cmax and AUC values in mice and significantly inhibits MAT2A in in vivo xenograft models, reducing tumor and brain SAM levels. It strongly binds to proteins in mouse plasma, with a low unbound fraction (Fu = 0.0028). Its potency is underscored by the plasma exposure required for SAM level reduction and its selectivity for tumor vs. brain reduction, as indicated by the free plasma IC50 ratio..
Note: Summary generated by AI. Data source: ChEMBL
Bioactivity
Description
AGI-43192 is a potent methionine adenosine transferase 2A (MAT2A) inhibitor that penetrates the blood-brain barrier. AGI-43192 inhibits S-adenosine methionine (SAM) production metabolic enzyme and methionine adenosine transferase 2A (MAT2A), which has the potential to study the role of SAM regulation in the central nervous system (CNS) and the treatment of cancer diseases.
Chemical Properties
Molecular Weight484.86
FormulaC23H16ClF3N6O
Cas No.2377491-54-6
SmilesCn1cc2cc(ccc2n1)-n1cc2cnc(NCC(F)(F)F)nc2c(-c2ccc(Cl)cc2)c1=O
Storage & Solubility Information
Storagestore at low temperature,keep away from direct sunlight | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
Solubility Information
DMSO: 45 mg/mL (92.81 mM), Sonication is recommended.
In Vivo Formulation
10% DMSO+40% PEG300+5% Tween 80+45% Saline: 8 mg/mL (16.5 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 mM2.0625 mL10.3123 mL20.6245 mL103.1226 mL
5 mM0.4125 mL2.0625 mL4.1249 mL20.6245 mL
10 mM0.2062 mL1.0312 mL2.0625 mL10.3123 mL
20 mM0.1031 mL0.5156 mL1.0312 mL5.1561 mL
50 mM0.0412 mL0.2062 mL0.4125 mL2.0625 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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