| Identification | Back Directory | [Name]
(S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(3,5-difluorophenyl)-5-oxopyrrolidine-2-carboxamide | [CAS]
1448346-43-7 | [Synonyms]
AGI14100
AGI-14100
AGI 14100
AGI-14100
(AGI14100)
(S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(3,5-difluorophenyl)-5-oxopyrrolidine-2-carboxamide | [Molecular Formula]
C29H22ClF4N5O3 | [MOL File]
1448346-43-7.mol | [Molecular Weight]
599.963 |
| Hazard Information | Back Directory | [Description]
AGI-14100 is a novel orally available mIDH1 inhibitor. Preclinical trials of AGI-14100 for the treatment of primary human myeloid leukemia therapy have been underway since 2013. | [Uses]
AGI-14100 is a metabolically stable and orally available mIDH1 inhibitor (IC50=6 nM). The pharmacochemical optimization of AGI-14100 is aimed at eliminating hPXR activation, resulting in the final drug candidate AG-120. AG-120 can be used in the study of cancers carrying IDH1 mutations. The discovery and development of AGI-14100 can be used for further studies of mutant isocitrate dehydrogenase 1 (mIDH1) inhibitors[1]. | [IC 50]
mIDH: 6 nM (IC50) | [References]
[1] Popovici-Muller J, et al. Discovery of AG-120 (Ivosidenib): a first-in-class mutant IDH1 inhibitor for the treatment of IDH1 mutant cancers[J]. ACS medicinal chemistry letters, 2018, 9(4): 300-305. DOI:10.1021/acsmedchemlett.7b00421 |
|
|