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Abiraterone (CB-7598) inhibits 17 α-hydroxylase/C17, 20 lyase (CYP17A1) with an IC50 of 4 nM, an enzyme which is expressed in testicular, adrenal, and prostatic tumor tissues. Abiraterone was recently approved for the treatment of docetaxel-treated castration-resistant prostate cancer (CRPC), is often effective, but requires coadministration with glucocorticoids to curtail side effects. Abiraterone inhibited in vitro proliferation and AR-regulated gene expression of AR-positive prostate cancer cells, which could be explained by AR antagonism in addition to inhibition of steroidogenesis.
| Cell Experiment | |
|---|---|
| Cell lines | PC-3 cells |
| Preparation method | Luciferase reporter assays We constructed a PSA-ARE3-luc luciferase reporter plasmid that was co-transfected with a human AR expression plasmid, F527-AR (wild-type (WT) or mutant as stated; mutations confirmed by sequencing (Beckman Coulter Genomics, UK)) into PC-3 cells. These were seeded in white opaque 384-well plates and grown in 10% CSS-supplemented phenol red-free RPMI 1640 for 30 hours. Cells were then treated with the indicated concentration of compound and R1881 for 16 hours. Luciferase activity was determined by adding ONE Glo (Promega, Southampton, UK) and measuring luminescence on a TopCount plate reader (Perkin-Elmer). |
| Concentrations | 0.1 - 25μM |
| Incubation time | 16 h |
| Animal Experiment | |
|---|---|
| Animal models | LAPC-4 xenograft with male SCID mice 4–6 weeks of age |
| Formulation | 0.3 % hydroxypropyl cellulose (HPC) in 0.9 % saline |
| Dosages | 0.15mM/kg bid |
| Administration | oral |
| Molecular Weight | 349.51 |
| Formula | C24H31NO |
| CAS Number | 154229-19-3 |
| Solubility (25°C) | DMF 6 mg/mL DMSO 2 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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