| Name | OT-82 |
| Description | OT-82 is a potent, selective, and orally active inhibitor of nicotinamide phosphoribosyltransferase (NAMPT). |
| In vitro | METHODS: OT-82 (0.001-10 μM) was used to treat human cell lines derived from HP and non-HP cancers, and the IC50 values were determined.
RESULTS: The average IC50 of OT-82 was significantly higher in non-HP cancer cells compared with HP cancer cells (13.03±2.94 nM vs 2.89±0.47 nM; p < 0.008). [1]
METHODS: MV4-11 cells were treated with OT-82 (0.001-10 nM), and the changes in NAD were observed for 24 hours, and the changes in ATP were observed for 24 hours and 48 hours.
RESULTS: OT-82 treatment resulted in a dose-dependent decrease in NAD and ATP concentrations in MV4-11 cells. OT-82 treatment of MV4-11 cells in vitro for 48 hours resulted in caspase-3 activation, an increase in the proportion of cells with sub-G1 DNA content, and mitochondrial membrane depolarization. OT-82 induced apoptosis and cell death by inhibiting NAMPT, leading to NAD and ATP depletion. [1] |
| In vivo | METHODS: OT-82 (25 or 50 mg/kg) was administered orally 6 days per week for 3 weeks. The therapeutic efficacy of OT-82 was tested in vivo using subcutaneous (SC) and systemic mouse xenograft models of HP malignancies.
RESULTS: OT-82 caused a dose-dependent inhibition of SC growth of human AML-derived MV4-11 cells; the 25 mg/kg dose resulted in a 3-fold reduction in mean tumor volume at day 17 of treatment, while higher doses resulted in complete eradication of tumors within 10 days of treatment initiation. [1] |
| Storage | Shipping with blue ice/Shipping at ambient temperature. |
| Solubility Information | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 3.3 mg/mL (7.77 mM), Sonication is recommended.
DMSO : 80 mg/mL (188.47 mM), Sonication is recommended.
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| Keywords | OT-82 | Nampt |
| Inhibitors Related | 10-Hydroxydecanoic Acid | Pendimethalin | N-Hydroxyphthalimide | Berberine hydrogen sulphate | Magnesium acetate tetrahydrate | 2-(1H-Indol-3-yl)ethan-1-ol | Cystamine dihydrochloride | Copper Sulfate Pentahydrate | (Iso)-Z-VAD(OMe)-FMK | Tauroursodeoxycholate | (E/Z)-10-Hydroxy-2-decenoic acid | Cinchonine |
| Related Compound Libraries | Bioactive Compound Library | Hematonosis Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | Fluorochemical Library | Anti-Cancer Compound Library | Anti-Cancer Active Compound Library | Anti-Cancer Drug Library |
United States
