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AGI-6780

Name: AGI-6780
Brand: TargetMol
SKU: T1809
Price: 31 USD
Availability: InStock
Rating: 5 (10 reviews)

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Catalog No. T1809Cas No. 1432660-47-3

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.

AGI-6780

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Purity: 99.7%

Catalog No. T1809Cas No. 1432660-47-3

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.

Pack Size	Price	USA Warehouse	Global Warehouse
1 mg	$31	In Stock	In Stock
2 mg	$44	In Stock	In Stock
5 mg	$72	In Stock	In Stock
10 mg	$122	In Stock	In Stock
25 mg	$232	In Stock	In Stock
50 mg	$413	In Stock	In Stock
100 mg	$618	In Stock	In Stock
500 mg	$1,330	-	In Stock
1 mL x 10 mM (in DMSO)	$77	In Stock	In 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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Batch Information

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Purity:99.7%

Appearance:Solid

Color:White

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COA HNMR LCMS

Product Introduction

Bioactivity

Description	AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant.
Targets&IC50	IDH2 (R140Q):23 nM
In vivo	AGI-6780 reverses differentiation blockage induced by IDH2/R140Q in TF-1 cells and induces rapid differentiation in primary samples from patients with IDH2/R140Q AML. It effectively reduces the levels of (R)-2-hydroxyglutarate (2-HG) in cell lines overexpressing ectopic IDH2/R140Q, with an EC50 of 20 nM, demonstrating excellent selectivity compared to other dehydrogenases.
Kinase Assay	AGI-6780 is prepared as 10 mM stock in DMSO and diluted to 50X final concentration in DMSO, for a 50 μL reaction mixture. IDH enzyme activity converting alpha-ketoglutarate to 2-hydroxyglutarate is measured using a NADPH depletion assay. In the assay the remaining cofactor is measured at the end of the reaction with the addition of a catalytic excess of diaphorase and resazurin, to generate a fluorescent signal in proportion to the amount of NADPH remaining. IDH enzyme activity in the direction of isocitrate to alpha-ketoglutarate conversion is measured by direct coupling of the NADPH production to conversion of resazurin to resorufin by diaphorase. In both cases, resorufin is measured fluorometrically at Ex544 Em590[1].
Cell Research	AGI-6780 is dissolved in DMSO and stored, and then diluted with appropriate media before use[1]. Cells are sorted from fresh or frozen bone marrow aspirates and blood samples after labelling with PE-CD34, APC-CD38, PE-CD14, FITC-CD3 (clone HIT3a) and PECy7-CD19 (clone SJ25C1) antibodies using a MoFlow cell sorter. Unfractionated nucleated blood or bone marrow cells are plated in Methocult H4434 methylcellulose medium at 104 cells/dish, in duplicate dishes per condition. AGI-6780 (5 mM) is directly added to the medium. Dishes are incubated in a humidified incubator at 37°C and colonies containing at least 30 cells are counted after 13 days[1].

Chemical Properties

Molecular Weight	481.51
Formula	C₂₁H₁₈F₃N₃O₃S₂
Cas No.	1432660-47-3
Smiles	FC(F)(F)c1cccc(NC(=O)Nc2cc(ccc2-c2ccsc2)S(=O)(=O)NC2CC2)c1
Relative Density.	1.52 g/cm3 (Predicted)

Storage & Solubility Information

Storage

In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 125 mg/mL (259.6 mM), Sonication is recommended.

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 89 mg/mL (184.84 mM), Sonication is recommended.

In Vivo Formulation

10% DMSO+40% PEG300+5% Tween 80+45% Saline: 3.3 mg/mL (6.85 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

	1mg	5mg	10mg	50mg
1 mM	2.0768 mL	10.3840 mL	20.7680 mL	103.8400 mL
5 mM	0.4154 mL	2.0768 mL	4.1536 mL	20.7680 mL
10 mM	0.2077 mL	1.0384 mL	2.0768 mL	10.3840 mL
20 mM	0.1038 mL	0.5192 mL	1.0384 mL	5.1920 mL
50 mM	0.0415 mL	0.2077 mL	0.4154 mL	2.0768 mL
100 mM	0.0208 mL	0.1038 mL	0.2077 mL	1.0384 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:

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 DMSO TargetMol | 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 DMSO TargetMol | reagent stock solution to 400 μL PEG300 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 ddH₂O TargetMol | 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.

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