Abiraterone Acetate (Zytiga; formerly CB-7598; CB7598; CB 7598)

Alias: Abiraterone Acetate; CB7630; CB 7630 ; CB-7630; trade name: Zytiga
Cat No.:V0801 Purity: ≥98%
Abiraterone Acetate (brand name Zytiga; formerly CB-7598; CB7598;CB 7598),the 3-acetylated and prodrug form of Abiraterone, is an irreversible and steroidal cytochrome CYP17 inhibitor with potential antitumor activity.
Abiraterone Acetate (Zytiga; formerly CB-7598; CB7598; CB 7598) Chemical Structure CAS No.: 154229-18-2
Product category: P450 (e.g. CYP)
This product is for research use only, not for human use. We do not sell to patients.
Size Price Stock Qty
10mg
50mg
100mg
500mg
1g
Other Sizes

Other Forms of Abiraterone Acetate (Zytiga; formerly CB-7598; CB7598; CB 7598):

  • Abiraterone
Official Supplier of:
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Top Publications Citing lnvivochem Products
InvivoChem's Abiraterone Acetate (Zytiga; formerly CB-7598; CB7598; CB 7598) has been cited by 1 publication
Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Abiraterone Acetate (brand name Zytiga; formerly CB-7598; CB7598; CB 7598), the 3-acetylated and prodrug form of Abiraterone, is an irreversible and steroidal cytochrome CYP17 inhibitor with potential antitumor activity. It inhibits CYP17 with an IC50 of 72 nM in a cell-free assay. Steroid CYP17/17alpha-monooxygenase is an enzyme involved in testosterone synthesis. Abiraterone acetate has been approved by the FDA in April 2011 for metastatic castration-resistant prostate cancer.

Biological Activity I Assay Protocols (From Reference)
ln Vitro
Abiraterone (Abi) acetate is an ester prodrug of the anticancer drug Abiraterone, with IC50 values for 17,20-lyase and 17α-hydroxylase (CYP17 is a bifunctional enzyme) with 17,20-lyase and 17α-hydroxylase activity of 15 nM and 2.5 nM, respectively. Abiraterone has an IC50 of 27 nM for human 17,20-lyase and 30 nM for 17α-hydroxylase inhibition[1]. The proliferation of AR-positive prostate cancer cell lines LNCaP and VCaP can be considerably inhibited by abiraterone at doses ≥ 5 μM, as demonstrated by research [2]. With competitive Ki values of 2.1 and 8.8 μM, abiraterone inhibits the activity of recombinant human 3βHSD1 and 3βHSD2. In both cell lines, 5α-diketone and DHT production could be totally inhibited by 10 μM abiraterone. In the rapidly expanding subgroup, biratterone treatment dramatically slowed the evolution of CRPC, effectively containing tumor growth for the entire 4-week treatment period (P<0.00001) [3].
ln Vivo
In prostate cancer that is resistant to castration, biratterone acetate (Abi) increases survival (CRPC). Abiraterone has been demonstrated to have an inhibitory dose of 0.5 mmol/kg/d, which results in serum concentrations of roughly 0.5 to 1 μM. It inhibits the consumption of [3H]-dehydroepiandrosterone (DHEA) and the buildup of Δ4-androstenedione (AD) in LNCaP with an IC50<1 μM. The control group's xenograft tumors showed a wide range of growth rates, with some growing slowly and only a few exhibiting vigorous growth [3].
Animal Protocol
Dissolved in 0.1 mL 5% benzyl alcohol and 95% safflower oil solution; 0.5 mmol/kg/d; s.c. injection
Male NOD/SCID mice with LAPC4 cells
References
[1]. Stein MN, et al. Androgen synthesis inhibitors in the treatment of castration-resistant prostate cancer. Asian J Androl. 2014 May-Jun;16(3):387-400.
[2]. Richards J, et al. 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.
[3]. Li R, et al. 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.
[4]. Lee GT, et al. Intracrine androgen biosynthesis in renal cell carcinoma. Br J Cancer. 2017 Mar 28;116(7):937-943.
[5]. A O'Donnell, et al. Hormonal impact of the 17α-hydroxylase/C17,20-lyase inhibitor abiraterone acetate (CB7630) in patients with prostate cancer. British Journal of Cancervolume 90, pages2317–2325 (2004)
These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C26H33NO2
Molecular Weight
391.55
CAS #
154229-18-2
SMILES
CC(O[C@H]1CC[C@]2(C)C3CC[C@]4(C)C(C5=CC=CN=C5)=CCC4C3CC=C2C1)=O
InChi Key
UVIQSJCZCSLXRZ-HMMZIKKISA-N
InChi Code
InChI=1S/C26H33NO2/c1-17(28)29-20-10-12-25(2)19(15-20)6-7-21-23-9-8-22(18-5-4-14-27-16-18)26(23,3)13-11-24(21)25/h4-6,8,14,16,20-21,23-24H,7,9-13,15H2,1-3H3/t20-,21?,23?,24?,25-,26+/m0/s1
Chemical Name
[(3S,10R,13S)-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
Synonyms
Abiraterone Acetate; CB7630; CB 7630 ; CB-7630; trade name: Zytiga
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 28 mg/mL (71.5 mM)
Water:<1 mg/mL
Ethanol:<1 mg/mL
Solubility (In Vivo)
5% DMSO+95% Corn oil: 30mg/mL
 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 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

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Abiraterone Acetate

  • Abiraterone Acetate

  • Abiraterone Acetate

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