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IDH889 is an orally available, brain permeable, allosteric and mutation-specific inhibitor of isocitrate dehydrogenase (IDH1). IDH889 showed high selectivity against IDH1R132 * mutant, with IC50 values of 0.02 μM, 0.072 μM and 1.38 μM against IDH1R132H, IDH1R132C and IDH1wt, respectively. IDH889 showed high inhibition of intracellular 2-Hg level with IC50 value of 0.014 μM.
| Molecular Weight | 436.48 |
| Formula | C23H25FN6O2 |
| CAS Number | 1429179-07-6 |
| Solubility (25°C) | DMSO ≥ 100 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Isocitrate Dehydrogenase (IDH) Products |
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| AGI-5198
AGI-5198 (IDH-C35) is the first highly potent and selective inhibitor of IDH1 R132H and R132C mutants in vitro with IC50 values of 0.07 μM and 0.16 μM, respectively. |
| AGI-6780
AGI-6780 is a potent and selective inhibitor of IDH2 R140Q mutant with IC50 of 23 nM. |
| Enasidenib
Enasidenib is an oral, potent, reversible, selective inhibitor of the IDH2 mutant enzymes, with IC50s of 100 and 400 nM against IDH2R140Q and IDH2R172K, respectively. |
| BAY-1436032
BAY1436032 is a novel pan-mutant IDH1 inhibitor, it specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells. |
| GSK864
GSK864 is a cell penetrant, potent and selective allosteric inhibitor of isocitrate dehydrogenase 1 (IDH1) that potently inhibits intracellular 2-hydroxyglutarate (2-HG) production in HT-1080 cells. |
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