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Ivosidenib is an orally available inhibitor of isocitrate dehydrogenase type 1 (IDH1), with potential antineoplastic activity. Ivosidenib specifically inhibits a mutated form of IDH1 in the cytoplasm, which inhibits the formation of the oncometabolite, 2-hydroxyglutarate (2HG).
In vitro, TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120.Treatment with AG-120 decreases intracellular 2-HG levels, inhibites growth factor independent proliferation and restores erythropoietin (EPO)-induced differentiation in TF-1 IDH1-R132H cells.
| Cell Experiment | |
|---|---|
| Cell lines | TF-1 cells |
| Preparation method | TF-1 cells or primary human AML patient samples expressing mutant IDH1 are treated with AG-120. |
| Concentrations | 0.5, 1.0, and 5.0 μM |
| Incubation time | 6 days |
| Animal Experiment | |
|---|---|
| Animal models | |
| Formulation | |
| Dosages | |
| Administration | |
| Molecular Weight | 582.96 |
| Formula | C28H22ClF3N6O3 |
| CAS Number | 1448347-49-6 |
| Solubility (25°C) | DMSO: ≥ 80 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 |
|---|
| 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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