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Rucaparib significantly potentiated TMZ-induced tumor regrowth delay in a flank tumor model of GBM12. Median time for tumor to exceed a 1000 mm3 size endpoint for placebo, TMZ, and TMZ/rucaparib treatment was 32, 86, and 121 days, p < 0.01, respectively. In contrast, the addition of rucaparib to TMZ therapy in GBM12 orthotopic xenografts was ineffective (median survival: placebo 16 days, TMZ 68 days and TMZ/rucaparib 81 days, p = 0.88. Therefore, subsequent studies focused on evaluating whether exclusion of rucaparib from the brain and orthotopic brain tumors might contribute to the lack of efficacy observed in the orthotopic xenograft models.
| Cell Experiment | |
|---|---|
| Cell lines | GBM12 cell |
| Preparation method | Cells were incubated with 2 −M rucaparib for 60 minutes at 37°C and then transport was quenched with cold PBS prior to lysis in 1% Triton X-100. Cell pellets were stored at −80°C until analysis using high-performance liquid chromatography followed by tandem mass spectrometry (LC-MS/MS). |
| Concentrations | 2 μM |
| Incubation time | 24 h |
| Animal Experiment | |
|---|---|
| Animal models | Mice with established intracranial xenografts |
| Formulation | dissolved in dimethylsulfoxide and diluted in saline |
| Dosages | 1 mg/kg |
| Administration | i.v. |
| Molecular Weight | 555.67 |
| Formula | C10H16O4S.C19H18FN3O |
| CAS Number | 1859053-21-6 |
| Form | Solid |
| Solubility (25°C) | 10 mM in DMSO |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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