AGI-6780

Catalog No.S7241

AGI-6780 Chemical Structure

Molecular Weight(MW): 481.51

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

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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

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]

Protocol

Solubility (25°C)

In vitro DMSO 96 mg/mL (199.37 mM)
Ethanol 96 mg/mL (199.37 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 481.51
Formula

C21 H18 F3 N3 O3 S2

CAS No. 1432660-47-3
Storage powder
Synonyms N/A

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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

Tel: +1-832-582-8158 Ext:3

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Dehydrogenase Signaling Pathway Map

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID