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Abiraterone acetate Cytochrome p450 17a1 inhibitor

Catalog No.A8202
Size Price Stock Qty
10mM (in 1mL DMSO)
$110.00
In stock
Evaluation Sample
$28.00
In stock
5mg
$120.00
In stock
50mg
$470.00
In stock

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Sample solution is provided at 25 µL, 10mM.

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Chemical structure

Abiraterone acetate

Related Biological Data

Abiraterone acetate

Related Biological Data

Abiraterone acetate

Biological Activity

Description Abiraterone Acetate, an acetate salt form of Abiraterone, is an inhibitor of steroidal cytochrome CYP17with IC50 of 72 nM.
Targets CYP17          
IC50 72 nM          

Protocol

Cell experiment [1]:

Cell lines

PC-3 cells

Preparation method

The solubility of this compound in DMSO is limited. General tips for obtaining a higher concentration: Please warm the tube at 37 °C for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below - 20 °C for several months.

Reacting condition

0.1 ~ 25 μM; 16 hrs

Applications

In PC-3 cells co-transfected with ARE3-luciferase and wild type or mutant androgen receptor (AR), Abiraterone Acetate at the dose up to 25 μM did not any obvious increase in luciferase activity. However, Abiraterone Acetate dose-dependently inhibited stimulated wild type and mutant AR activity, with significant inhibition observed at the doses ≤ 10 μM.

Animal experiment [2]:

Animal models

Male NOD/SCID mice bearing LAPC4 cells

Dosage form

0.5 mmol/kg/d; i.p.; 5 days per week, for 4 weeks

Applications

Abiraterone Acetate at the dose of 0.5 mmol/kg/d resulted in serum concentrations ranging from 0.5 to 1 mmol/L. Compared with the control group, Abiraterone Acetate treatment significantly inhibited "castration-resistant" prostate cancer progression in the robustly growing subset, effectively inhibiting tumor growth over 4 weeks of treatment.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

[1]. Richards J, Lim AC, Hay CW, Taylor AE, Wingate A, Nowakowska K, Pezaro C, Carreira S, Goodall J, Arlt W, McEwan IJ, de Bono JS, Attard G. Interactions of abiraterone, eplerenone, and prednisolone with wild-type and mutant androgen receptor: a rationale for increasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82.

[2]. Li R, Evaul K, Sharma KK, Chang KH, Yoshimoto J, Liu J, Auchus RJ, Sharifi N. Abiraterone inhibits 3β-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistant prostate cancer. Clin Cancer Res. 2012 Jul 1;18(13):3571-9.

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Chemical Properties

Cas No. 154229-18-2 SDF Download SDF
Chemical Name [(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-pyridin-3-yl-2,3,4,7,8,9,11,12,14,15-decahydro-1H-cyclopenta[a]phenanthren-3-yl] acetate
Canonical SMILES CC(=O)OC1CCC2(C3CCC4(C(C3CC=C2C1)CC=C4C5=CN=CC=C5)C)C
Formula C26H33NO2 M.Wt 391.55
Solubility Limited solubility Storage Store at -20°C
Shipping Condition Evaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Background

Abiraterone acetate is the 3β-acetate form of its active component abiraterone, a potent inhibitor of androgen biosynthesis. Abiraterone, a pregnenolone-derived 3-pyridyl steroidal compound, potently and irreversibly inhibits cytochrome P450 17 alpha-hydroxylase (CYP17), an important enzyme involved in the synthesis of androgen and cortisol, through a covalent binding mechanism with a value of 50% inhibition concentration IC50 of 72 nM, which is 10 to 30 times greater in potency, due to the 3-pyridyl substitution in its chemical structure, than the inhibition by ketoconazole. In order to improve the low solubility of abirateone, abiraterone acetate has been developed and used for the treatment of castration-resistant prostate cancer (CRPC).

Reference

Charles J Ryan and Michael L Cheng. Abiraterone acetate for the treatment of prostate cancer. Expert Opin. Pharmacother. (2013) 14 (1): 91-96

Tadas S. Vasaitis, Robert D. Bruno and Vincent C.O. Njar. CYP17 inhibitors for prostate cancer therapy. Journal of Steroid Biochemistry & Molecular Biology 125 (2011) 23-31

Guru Sonpavde, Gerhardt Attard, Joaquim Bellmunt, Malcolm D. Mason, Bernard Malavaud, Bertrand Tombal and Cora N. Sternberg. The role of abiraterone acetate in the management of prostate cancer: a critical analysis of the literature. EUROPEAN UROLOGY 60 (2011) 270-278