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BAY1436032 is a novel pan-mutant IDH1 inhibitor, it specifically inhibits R-2HG production and colony growth, and induces myeloid differentiation of AML cells.
In vitro: BAY1436032 inhibited intracellular R-2HG production in mouse hematopoietic cells expressing IDH1R132H or IDH1R132C with an IC50 of 60 and 45 nm, respectively. In contrast, R-2HG levels were not reduced in IDH2R140Q and IDH2R172K expressing mouse hematopoietic cells by BAY1436032 at concentrations up to 10 μm.
In vivo: Treatment with vehicle or 150 mg/kg BAY1436032 once daily by oral gavage was initiated at day 15 after transplantation. BAY1436032 and vehicle-treated mice had similar percentages of hCD45+ cells, peripheral blood counts, spleen weight at death and survival, confirming the on-target activity of BAY1436032
| Cell Experiment | |
|---|---|
| Cell lines | HoxA9-IDH1R132 cell lines |
| Preparation method | Vehicle or BAY1436032 was added to methylcellulose containing 105 human mononuclear cells, which were plated in duplicate. Colonies were evaluated microscopically 10 to 14 days after plating by standard criteria. |
| Concentrations | 0.1 μm |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | NSG mice |
| Formulation | DMSO |
| Dosages | 45 or 150 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 489.53 |
| Formula | C26H30F3N3O3 |
| CAS Number | 1803274-65-8 |
| Solubility (25°C) | DMSO 90 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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