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AR-42 is a novel HDAC inhibitor with an IC50 of 0.61 μM for acute lymphoblastic leukemia (697) cell lines. In chronic lymphocytic leukemia (CLL) cells, the 48-hr LC50 of AR-42 is 0.76 μM. AR-42 produces dose- and time-dependent acetylation both of histones and tubulin, and induces caspase-dependent apoptosis that is not reduced in the presence of stromal cells. AR-42 significantly reduced leukocyte counts and/or prolonged survival in three separate mouse models of B-cell malignancy without evidence of toxicity. AR-42 has in vitro and in vivo efficacy at tolerable doses. In additon, AR-42 promoted hyperacetylation of H3, H4, and alpha-tubulin, and up-regulation of p21.
| Cell Experiment | |
|---|---|
| Cell lines | DU-145 |
| Preparation method | Cells are exposed to varous concentrations of AR-42 for 96 hours. The medium is removed and replaced by 150 μL of 0.5 mg/mL of MTT in RPMI 1640 medium, and the cells are incubated in the CO2 incubator at 37 °C for 2 hours. Supernatants are removed from the wells, and the reduced MTT dye is solubilized with 200 μL/well of DMSO. Absorbance is determined on a plate reader at 570 nm. |
| Concentrations | Dissolved in DMSO, final concentrations ~2.5 μM |
| Incubation time | 96 hours |
| Animal Experiment | |
|---|---|
| Animal models | Intact male NCr athymic nude mice inoculated s.c. with PC-3 cells |
| Formulation | Formulated in methylcellulose/Tween 80 |
| Dosages | ~50 mg/kg/day |
| Administration | Orally |
| Molecular Weight | 312.36 |
| Formula | C18H20N2O3 |
| CAS Number | 935881-37-1 |
| Solubility (25°C) | DMSO 20 mg/mL Ethanol 50 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[3] Sophia G Liva, et al. Phase I study of AR-42 and decitabine in acute myeloid leukemia
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