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10mg |
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50mg |
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100mg |
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500mg |
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1g |
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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. 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.
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].
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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].
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Animal Protocol |
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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) |
Molecular Formula |
C26H33NO2
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Molecular Weight |
391.55
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CAS # |
154229-18-2
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SMILES |
CC(O[C@H]1CC[C@]2(C)C3CC[C@]4(C)C(C5=CC=CN=C5)=CCC4C3CC=C2C1)=O
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InChi Key |
UVIQSJCZCSLXRZ-HMMZIKKISA-N
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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
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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
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Synonyms |
Abiraterone Acetate; CB7630; CB 7630 ; CB-7630; trade name: Zytiga
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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)
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Solubility (In Vitro) |
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Solubility (In Vivo) |
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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.
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.