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Unesbulin (PTC596) is a novel orally active and selective B-cell-specific Moloney murine leukemia virus integration site 1 (BMI-1) inhibitor, Unesbulin downregulating MCL-1 and inducing p53-independent mitochondrial apoptosis in acute myeloid leukemia progenitor cells.
Unesbulin (10 or 12.5 mg/kg; oral gavage; twice a week until death) causes the survival significantly longer than the vehicle-treated group in NOD-SCID mice with HL-60 cells.
| Cell Experiment | |
|---|---|
| Cell lines | Z-138 and REC-1 cells |
| Preparation method | Z-138 and REC-1 cells were treated for 24 hours with 300 nM PTC596, after which BCL-2, BCL-XL and MCL-1 protein levels were determined. |
| Concentrations | 300 nM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Non-obese diabetic-severe combined immunodeficiency (NOD-SCID)/IL2Rγ-KO (NSG) mice |
| Formulation | 0.5% hydroxypropyl methylcellulose and 0.1% Tween 80 in distilled water |
| Dosages | 5 mg/kg |
| Administration | oral gavage |
| Molecular Weight | 420.34 |
| Formula | C19H13F5N6 |
| CAS Number | 1610964-64-1 |
| Form | Solid |
| Solubility (25°C) | DMSO 9 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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