Home Metabolism Dehydrogenase inhibitor AGI-6780 For research use only.

AGI-6780

AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.

AGI-6780 Chemical Structure

AGI-6780 Chemical Structure

CAS No. 1432660-47-3

Purity & Quality Control

AGI-6780 Related Products

Signaling Pathway

Dehydrogenase Signaling Pathways

Dehydrogenase Signaling Pathway

Biological Activity

Description AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM.
Targets
IDH2 R140Q mutant [1]
23 nM
In vitro
In vitro AGI-6780 potently reduce (R)-2-hydroxyglutarate (2HG) levels in cell lines ectopically overexpressing IDH2/R140Q with EC50 of 20 nM, with excellent selectivity against other dehydrogenases. AGI-6780 reverses the IDH2/R140Q-induced differentiation block in TF-1 cells, and induces blast differentiation in primary human IDH2/R140Q AML patient samples. [1]

Chemical Information & Solubility

Molecular Weight 481.51 Formula

C21 H18 F3 N3 O3 S2
CAS No. 1432660-47-3 SDF Download AGI-6780 SDF
Smiles C1CC1NS(=O)(=O)C2=CC(=C(C=C2)C3=CSC=C3)NC(=O)NC4=CC=CC(=C4)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 96 mg/mL ( (199.37 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 96 mg/mL

Water : Insoluble


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In vivo
Batch:

Add solvents to the product individually and in order.


In vivo Formulation Calculator

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In vivo Formulation Calculator (Clear solution)

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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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