AGI 5198
Chemical Name: N-[2-(Cyclohexylamino)-1-(2-methylphenyl)-2-oxoethyl]-N-(3-fluorophenyl)-2-methyl-1H-Imidazole-1-acetamide
Purity: ≥98%
Biological Activity
AGI 5198 is a potent and selective inhibitor of mutant isocitrate dehydrogenase 1 (mIDH1; IC50 = 70 nM). Selective for mIDH1 over wild-type IDH1 and IDH2. Inhibits production of oncometabolite D-2 hydroxyglutarate. Attenuates growth of glioma cells containing mIDH1, but not wild-type IDH1, in vitro and in vivo. Also inhibits growth of fibrosarcoma and chondrosarcoma cells bearing mIDH1.Technical Data
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Background References
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An inhibitor of mutant IDH1 delays growth and promotes differentiation of glioma cells.
Rohle et al.
Science, 2013;340:626 -
Treatment with a small molecule mutant IDH1 inhibitor suppresses tumorigenic activity and decreases production of the oncometabolite 2-hydroxyglutarate in human chondrosarcoma cells.
Li et al.
PLoS ONE, 2015;10:e0133813 -
Oncogenic R132 IDH1 mutations limit NADPH for de novo lipogenesis through (D)2-hydroxyglutarate production in fibrosarcoma cells.
Badur et al.
Cell Rep., 2018;25:1018
Product Datasheets
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