In vitro: Salermide prompts tumour-specific cell death in a wide range of human cancer cell lines. The antitumour activity of Salermide is primarily because of a massive induction of apoptosis. Salermide induces apoptosis in cancer but not in normal cells. It induces strong apoptosis without any evident effect on the cell cycle in all the cancer cell lines analysed except in non-tumorigenic MRC5 cells. The induction of apoptosis is cell-type-specific and dose-dependent. In vivo: Salermide is well tolerated by mice at concentrations up to 100 μM. Its feeding does not produce any adverse health effects in mice as monitored by diet consumption, body-weight gain, and postural and behavioural changes.
| Cell Experiment | |
|---|---|
| Cell lines | Cell lines: MOLT4, MDA-MB-231 and SW480 cancer cell lines |
| Preparation method | Cell viability is determined using the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide assay as described earlier. IC50 index is calculated using four Salermide concentrations (25, 50, 75 and 100 μm) for 24 h. The percentage of apoptotic cells is determined with the FACSCalibur apparatus. |
| Concentrations | 0, 25, 50, 75 or 100 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Athymic (BALB/c, nu/nu) female nude mice |
| Formulation | |
| Dosages | 100 μl of 100 μM |
| Administration | i.p. |
| Molecular Weight | 394.47 |
| Formula | C26H22N2O2 |
| CAS Number | 1105698-15-4 |
| Form | Solid |
| Solubility (25°C) | 78 mg/mL in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Species | Mouse | Rat | Rabbit | Guinea pig | Hamster | Dog |
| Weight (kg) | 0.02 | 0.15 | 1.8 | 0.4 | 0.08 | 10 |
| Body Surface Area (m2) | 0.007 | 0.025 | 0.15 | 0.05 | 0.02 | 0.5 |
| Km factor | 3 | 6 | 12 | 8 | 5 | 20 |
| Animal A (mg/kg) = Animal B (mg/kg) multiplied by | Animal B Km |
| Animal A Km |
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
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