Skip to main content
. 2022 Jun 7;38(9):1069–1084. doi: 10.1007/s12264-022-00866-1

Table 2.

Mutant IDH Inhibitors

Drug names Structure Introductions
AGI-5198 graphic file with name 12264_2022_866_Figa_HTML.gif AGI-5198 (IDH-C35) is the first highly effective and selective mutant IDH1 inhibitor, with an IC50 = 0.07 and 0.16 μmol/L for IDH1R132H and IDH1R132C, respectively.
IDH1 Inhibitor 3 graphic file with name 12264_2022_866_Figb_HTML.gif IDH1 Inhibitor 3 is a mutant IDH1 inhibitor, with an IC50 of 45 nmol/L for IDH1R132H.
IDH-889 graphic file with name 12264_2022_866_Figc_HTML.gif IDH-305 is an oral and brain-penetrating inhibitor of mutant IDH1, with an IC50 = 0.02, 0.072, and 1.38 mol/L for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively.
Mutant IDH1-IN-1 graphic file with name 12264_2022_866_Figd_HTML.gif Mutant IDH1-IN-1 is a selective inhibitor of mutant IDH1R132H, with IC50 = 81.5 nmol/L.
α-Mangostin graphic file with name 12264_2022_866_Fige_HTML.gif α-Mangostin is an inhibitor of mutant IDH1R132H with a Ki of 2.85 μmol/L; IC50 = 2.85 μmol/L.
FT-2102 graphic file with name 12264_2022_866_Figf_HTML.gif FT-2102 is a mutant IDH1 inhibitor, with an IC50 = 9 and 39 nmol/L for IDH1R132H and IDH1R132C, respectively, in U87 glioma cells.
AGI-6780 graphic file with name 12264_2022_866_Figg_HTML.gif IDH2/R140Q mutation inhibitor
IDH-305 graphic file with name 12264_2022_866_Figh_HTML.gif IDH-305 is an oral and brain-penetrating inhibitor of mutant IDH1, with an IC50 = 27, 28, and 6,140 nmol/L for recombinant IDH1R132H, IDH1R132C, and wild-type IDH1, respectively.
DS-1001b graphic file with name 12264_2022_866_Figi_HTML.gif Seen in the main manuscript
BAY-1436032 graphic file with name 12264_2022_866_Figj_HTML.gif Seen in the main manuscript
AG-120 graphic file with name 12264_2022_866_Figk_HTML.gif Seen in the main manuscript
(R,S)-AG-120 graphic file with name 12264_2022_866_Figl_HTML.gif Seen in the main manuscript
AG-221 graphic file with name 12264_2022_866_Figm_HTML.gif Seen in the main manuscript
AG-881 graphic file with name 12264_2022_866_Fign_HTML.gif Seen in the main manuscript