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IDH2-C100 is a potent and selective inhibitor of IDH2 R140Q and R172K mutant first reported in patent WO 2013102431. It can inhibit the enzymatic activity of IDH2 R140Q and R172K in vitro with an IC₅₀ < 0.1 µM. It has IC₅₀ < 0.1 µM in U87MG pLVX-IDH2 R140Q-neo cell based assay. It is an analog of clinical IDH2 inhibitor AG-221 by Thomson Reuters Integrity analysis.

How to Use:

• In vitro: IDH2-C100 was used at 1-5 µM in vitro and cellular assays.
• In vivo: n/a

Reference:

• 1. Giovanni Cianchetta, et al. Therapeutically active compounds and their methods of use. (2013) PCT WO 2013102431