1. Metabolic Enzyme/Protease
  2. Cytochrome P450
  3. Abiraterone

Abiraterone (Synonyms: CB-7598)

Cat. No.: HY-70013 Purity: 99.61%
Handling Instructions

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.

For research use only. We do not sell to patients.

Abiraterone Chemical Structure

Abiraterone Chemical Structure

CAS No. : 154229-19-3

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Customer Review

Based on 7 publication(s) in Google Scholar

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Description

Abiraterone is a potent and irreversible CYP17A1 inhibitor with antiandrogen activity, which inhibits both the 17α-hydroxylase and 17,20-lyase activity of the cytochrome p450 enzyme CYP17 with IC50s of 2.5 nM and 15 nM, respectively.

IC50 & Target

IC50:17α-hydroxylase (2.5 nM), 17,20-lyase (15 nM)[6]

In Vitro

Significant inhibition of proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP with doses of Abiraterone ≥5 μM is confirmed[2]. Abiraterone shows IC50 values of 15 nM and 2.5 nM for the 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17α-hydroxylase with IC50 of 27 and 30 nM respectively[3]. Abiraterone inhibits recombinant human 3βHSD1 and 3βHSD2 activity with competitive Ki values of 2.1 and 8.8 μM. 10 μM Abiraterone is sufficient to completely block synthesis of 5α-dione and DHT in both cell lines.Treatment with abi significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001). [3H]-dehydroepiandrosterone (DHEA) depletion and Δ4-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC50<1 μM[4].

In Vivo

The 0.5 mmol/kg/d Abiraterone treatment dose is previously shown to yield serum concentrations of about 0.5 to 1 μM. Xenograft tumor growth in the control group is widely variable, with some tumors growing slowly and only a subset of tumors exhibiting robust growth[4]. Following i.v. administration (5 mg/kg) the clearance (Cl) and volume of distribution (Vd) are found to be 31.2 mL/min/kg and 1.97 L/kg, respectively. The AUC0-∞ (area under the plasma concentration-time curve from time zero to infinity time point) is found to be 2675 ng*h/mL. The terminal half-life (t1/2) is 0.73 h. Because of high clearance, Abiraterone (ART) is quantifiable only until 2 h following i.v. administration[5].

Clinical Trial
Molecular Weight

349.51

Formula

C₂₄H₃₁NO

CAS No.

154229-19-3

SMILES

C[[email protected]@]12C(C3=CN=CC=C3)=CC[[email protected]]1([[email protected]@]4(CC=C5[[email protected]@](C)([[email protected]]4(CC2)[H])CC[[email protected]@H](C5)O)[H])[H]

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Solvent & Solubility
In Vitro: 

DMF : 8.75 mg/mL (25.04 mM; Need ultrasonic and warming)

Ethanol : 5.4 mg/mL (15.45 mM; Need ultrasonic)

DMSO : 5 mg/mL (14.31 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.8611 mL 14.3057 mL 28.6115 mL
5 mM 0.5722 mL 2.8611 mL 5.7223 mL
10 mM 0.2861 mL 1.4306 mL 2.8611 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free or FBS-supplemented media for 7 days. Cells are treated with Abiraterone (5 μM and 10 μM) at 24 and 96 hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuring luminescence[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[4][5]

Mice[4]
Male NOD/SCID mice 6 to 8 weeks of age are surgically orchiectomized and implanted with a 5 mg 90-day sustained release DHEA pellet to mimic CRPC with human adrenal physiology. Two days later, 7×106 LAPC4 cells are injected subcutaneously with Matrigel. Tumor dimensions are measured 2 to 3 times per week, and volume is calculated as length×width×height×0.52. Once tumors reach 300 mm3, mice are randomly assigned to vehicle or Abiraterone treatment groups. Mice in the Abiraterone group are treated with 5 mL/kg intraperitoneal injections of 0.5 mmol/kg/d (0.1 mL 5% benzyl alcohol and 95% safflower oil solution) and control mice with vehicle only, once daily for 5 days per week over a duration of 4 weeks (n=8 mice per treatment). Statistical significance between Abiraterone and vehicle treatment groups is assessed by ANOVA based on a mixed-effect model.
Rats[5]
Male Sprague-Dawley rats (n=8, 240-260 g) are used. Blood samples (450 µL) are obtained following an i.v. 5 mg/kg dose of ART into polypropylene tubes containing Na2-EDTA solution as an anticoagulant and at pre-dose, 0.12, 0.25, 0.5, 1, 2, 4, 6, 8 and 24 h (a sparse sampling protocol is adopted during blood collection and at each time point blood is collected from four animals). Plasma is harvested by centrifuging the blood using a Biofuge at 1760g for 5 min and stored frozen at -80±10°C until analysis.

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.61%

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Abiraterone
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HY-70013
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