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Lurbinectedin, also known as PM01183, is a marine-derived covalent DNA binder with potential antineoplastic activity. Lurbinectedin (PM01183) covalently binds to residues lying in the minor groove of DNA, which may result in delayed progression through S phase, cell cycle arrest in the G2/M phase and cell death. Lurbinectedin significantly inhibits tumor growth in a mouse CCC cell xenografts.
| Cell Experiment | |
|---|---|
| Cell lines | CCC cells |
| Preparation method | CCC cells (2×105) were incubated with lurbinectedin at the indicated concentrations for 48 hours. The cells were then fixed with 75% ethanol overnight at -20°C and stained with propidium iodide (PI; 50 μg/mL) in the presence of RNase A (100 μg/mL; Roth) for 60 minutes at 4°C. In each experiment, the cell cycle distribution was determined by analyzing 10,000 cells using a FACScan flow cytometer and Cell Quest software (Becton Dickinson, NJ, USA), as reported previously. |
| Concentrations | - |
| Incubation time | 48 hours |
| Animal Experiment | |
|---|---|
| Animal models | Five- to 7-week-old nude mice injected RMG1 cells |
| Formulation | - |
| Dosages | 0.180 mg/kg |
| Administration | i.v. administered each week for 6 weeks |
| Molecular Weight | 784.87 |
| Formula | C41H44N4O10S |
| CAS Number | 497871-47-3 |
| Solubility (25°C) | DMSO 1 μmol/L |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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