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Oleandrin
| Product Name | Oleandrin |
| Price: | $146 / 20mg |
| Catalog No.: | CN02527 |
| CAS No.: | 465-16-7 |
| Molecular Formula: | C32H48O9 |
| Molecular Weight: | 576.7 g/mol |
| Purity: | >=98% |
| Type of Compound: | Steroids |
| Physical Desc.: | Powder |
| Source: | The herbs of Nerium oleander L. |
| Solvent: | DMSO, Pyridine, Methanol, Ethanol, etc. |
| SMILES: | CO[C@H]1C[C@H](O[C@H]2CC[C@]3([C@@H](C2)CC[C@@H]2[C@@H]3CC[C@]3([C@]2(O)C[C@@H]([C@@H]3C2=CC(=O)OC2)OC(=O)C)C)C)O[C@H]([C@@H]1O)C |
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| Description | Oleandrin inhibits the Na+, K+-ATPase activity with an IC50 of 620 nM. |
| Target | IC50: 620 nM (Na+, K+-ATPase)[1]. |
| In Vitro | Study of Na,K-ATPase inhibition shows an IC50 (nM) of 620 for Oleandrin. The inhibition of Na,K-ATPase by Oleandrin confirms that it likely exert its toxic effect through inhibition of sodium pump activity[1]. When treated with a series of concentrations of Oleandrin (0.2-25 nM), the undifferentiated CaCO-2 cells are sensitive as evidenced by an IC50 of 8.25 nM. In contrast, a maximum growth inhibition of only 20% is reached in differentiated CaCO-2 cells even though they are treated with Oleandrin concentrations as high as 25 nM[2]. |
| In Vivo | The effect of Oleandrin is investigated on glioma growth in vivo. To this aim, SCID or C57BL/6 mice are transplanted, respectively, with human U87MG (5×104), U251, GBM19 (5×105), or murine (syngeneic) GL261 (7.5×104) cells into the right striatum and, after 10 d, treated daily with intraperitoneal Oleandrin for an additional 7 d. Oleandrin significantly reduces tumor sizes in human and murine glioma cell models in vivo in a dose-dependent way. High concentrations of Oleandrin (3 mg/kg) are fatal in both models, as expected from the known lethal dose for rodents. Doses of Oleandrin below the lethal dose (0.3 mg/kg) significantly increase the survival time from 32.6±1.4 d to 53.8±9.6 d in mice injected with U87MG cells (n=5-11; p<0.01, log-rank test) and from 23.37±1.2 d to 34.38±3.3 d (n=5-11; p<0.01, log rank test) in mice injected with GL261 cells[3]. |
| Cell Assay | Undifferentiated wild-type and well-differentiated CaCO-2 cells are treated with a range of concentrations of Oleandrin (0.2-25 nM). After 48 h, cells are labeled with BrdU and relative cell proliferation is determined with a BrdU Cell Proliferation Kit[2]. |
| Animal Admin | Mice[3] After tumor cell injection, SCID or C57BL/6 mice are monitored daily. The end point is determined by lack of physical activity or death. The mean survival time is calculated using the Kaplan-Meier method and statistical analysis is performed using a log-rank test. For cotreatment with Temozolomide (TMZ), 10 d after tumor injection, mice are treated with Oleandrin (0.03, 0.3, or 3 mg/kg/daily, i.p.), TMZ (50 mg/kg, i.p., every 2 d for a total of 4 times with a stop of 2 weeks) or both. The dosing scheme is chosen starting from these data to be reasonably sure that a constant concentration of drug is maintained along the experiment. Animals used in Kaplan-Meier survival studies receive up to four TMZ cycles. |
| Density | 1.26 |
| Boiling Point | 693.7±55.0 °C at 760 mmHg |
| Flash Point | 217.2±25.0 °C |
| Exact Mass | 576.329834 |
| PSA | 120.75000 |
| LogP | 2.30 |
| Vapour Pressure | 0.0±4.9 mmHg at 25°C |