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Lomustine (CeeNU) is an alkylating agent of value against both hematologic malignancies and solid tumors. Lomustine is a highly lipophilic nitrosourea compound which undergoes hydrolysis in vivo to form reactive metabolites. These metabolites cause alkylation and cross-linking of DNA. Other biologic effects include inhibition of DNA synthesis and some cell cycle phase specificity. Nitrosureas generally lack cross-resistance with other alkylating agents.
| Cell Experiment | |
|---|---|
| Cell lines | XP cells |
| Preparation method | Growing cell lines routinely as monolayers in DMEM supplemented with 10% foetal calf serum, 25 mm HEPES, glutamine and penicillin/streptomycin. Carrying cytotoxicity studies out in HEPES-free medium in a 5% CO2 atmosphere. Plating 750-1000 cells/well in 96 well plates and after overnight incubation,treating them for 2 hours with or without 33 μM BG. Then adding temozolomide or CCNU for 1 hour in the same medium, the final DMSO concentration not exceeding 1%. Growing the cells for a further 7 days in fresh medium and assaying for protein content by the NCI sulphorhodamine assay; growth studies show that during the assay period cells are in log phase growth . For the repeat temozolomide dosing schedule, cells are given consecutive 24 hours treatments, with fresh medium each day. Carrying assays out at least in duplicate. |
| Concentrations | 133 μM |
| Incubation time | 1 hour |
| Animal Experiment | |
|---|---|
| Animal models | Dogs |
| Formulation | Saline |
| Dosages | 90 mg/m2 |
| Administration | Orally |
| Molecular Weight | 233.7 |
| Formula | C9H16ClN3O2 |
| CAS Number | 13010-47-4 |
| Form | Solid |
| Solubility (25°C) | DMSO 40 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
[2] Alaaeddin Alrohaibani, et al. Microangiopathy, lomustine, and karyomegalic mesangial cells
[3] Michael Weller, et al. How did lomustine become standard of care in recurrent glioblastoma?
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