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Abiraterone

Cat. No. M1636
Abiraterone Structure
Synonym:

CB-7598

Size Price Availability Quantity
Free Sample (0.5-1 mg)  USD 0 In stock
10mM*1mL in DMSO USD 70  USD70 In stock
10mg USD 63  USD63 In stock
50mg USD 145  USD145 In stock
100mg USD 220  USD220 In stock
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Quality Control & Documentation
Biological Activity

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.

Protocol (for reference only)
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
Chemical Information
Molecular Weight 349.51
Formula C24H31NO
CAS Number 154229-19-3
Solubility (25°C) DMSO
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Richards et al. Cancer Res. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100.

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Keywords: Abiraterone, CB-7598 supplier, Cytochrome P450 (e.g. CYP17), inhibitors, activators


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