1. Metabolic Enzyme/Protease
  2. Cytochrome P450

Abiraterone acetate (Synonyms: CB7630)

Cat. No.: HY-75054 Purity: 99.92%
Handling Instructions

Abiraterone acetate is an oral, potent, selective, and irreversible inhibitor of CYP17.

For research use only. We do not sell to patients.
Abiraterone acetate Chemical Structure

Abiraterone acetate Chemical Structure

CAS No. : 154229-18-2

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Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
10 mg USD 60 In-stock
50 mg USD 74 In-stock
100 mg USD 96 In-stock
200 mg USD 120 In-stock
500 mg USD 144 In-stock
1 g USD 180 In-stock
2 g USD 288 In-stock
5 g USD 528 In-stock
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Other Forms of Abiraterone acetate:

    Abiraterone acetate purchased from MCE. Usage Cited in: Br J Cancer. 2017 Mar 28;116(7):937-943.

    Targeting the androgen signaling axis decreases tumour growth in AR-positive human RCC cell line, Caki2, xenografts. (A) After inoculating the flanks with Caki2, 30 mice are randomized into six groups of five mice each. The treatment is rendered as indicated. Both enzalutamide (Enz) and Abiraterone acetate (AA) decrease tumor volume dramatically. (B) Gross picture of tumors collected from mice after treatment. (C) After establishing the tumors, 30 mice are surgically castrated and treated with t
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

    Abiraterone acetate is an oral, potent, selective, and irreversible inhibitor of CYP17.

    IC50 & Target

    CYP17[1]

    In Vitro

    Abiraterone (Abi) acetate is an ester prodrug of the anticancer agent Abiraterone, which 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[1]. 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 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 Abiraterone significantly inhibited CRPC progression in the robustly growing subset, effectively putting a ceiling on tumor growth over 4 weeks of treatment (P<0.00001)[3].

    In Vivo

    Abiraterone (Abi) acetate prolongs survival in castration-resistant prostate cancer (CRPC). [3H]-dehydroepiandrosterone (DHEA) depletion and Δ4-androstenedione (AD) accumulation are inhibited by Abiraterone in LNCaP, with an IC50<1 μM. 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[3].

    References
    Preparing Stock Solutions
    Concentration Volume Mass 1 mg 5 mg 10 mg
    1 mM 2.5540 mL 12.7698 mL 25.5395 mL
    5 mM 0.5108 mL 2.5540 mL 5.1079 mL
    10 mM 0.2554 mL 1.2770 mL 2.5540 mL
    Please refer to the solubility information to select the appropriate solvent.
    Cell Assay
    [2]

    Abiraterone acetate is dissolved in DMSO and then diluted to a maximum DMSO concentration of 0.2%[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
    [3]

    Abiraterone acetate is prepared in 0.1 mL 5% benzyl alcohol and 95% safflower oil solution[3].

    Mice[3]
    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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    391.55

    Formula

    C₂₆H₃₃NO₂

    CAS No.

    154229-18-2

    SMILES

    O=C(O[[email protected]@H]1CC2=CC[[email protected]]3([H])[[email protected]]([H])(CC[[email protected]](C)(C(C4=CN=CC=C4)=CC5)[[email protected]]35[H])[[email protected]@]2(C)CC1)C

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Solvent & Solubility

    10 mM in DMSO

    Abiraterone acetate is prepared in 0.1 mL 5% benzyl alcohol and 95% safflower oil solution[4].

    * "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

    References

    Purity: 99.92%

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    Inquiry Information

    Product Name:
    Abiraterone acetate
    Cat. No.:
    HY-75054
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