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| 100mg |
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| 250mg |
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| 500mg |
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Purity: ≥98%
Abiraterone (formerly also known as CB 7598; CB7598; CB-7598; trade name Zytiga) is a novel, higly potent, irreversible and selective CYP17 inhibitor with potential antineoplastic activity. It inhibits CYP17 with an IC50 of 2 nM in a cell-free assay. Abiraterone is an approved drug used in combination with a corticosteroid for metastatic castration-resistant prostate cancer and metastatic high-risk castration-sensitive prostate cancer.
| ln Vitro |
It has been established that dosages of Abiraterone ≥5 μM significantly limit the proliferation of the AR-positive prostate cancer cell lines LNCaP and VCaP[2]. For both 17,20-lyase and 17α-hydroxylase, abiraterone has IC50 values of 15 nM and 2.5 nM (CYP17 is a bifunctional enzyme with both 17α-hydroxylase and 17,20-lyase activity). Human 17,20-lyase and 17α-hydroxylase are inhibited by abiraterone, with IC50 values of 27 and 30 nM, respectively[3]. 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, 10 μM abiraterone is enough to totally prevent the synthesis of DHT and 5α-dione. In the robustly growing fraction, treatment with abi substantially slowed the progression of CRPC, effectively capping tumor growth throughout the course of four weeks of treatment (P<0.00001). Abiraterone inhibits the buildup of Δ4-androstenedione (AD) and the depletion of [3H]-dehydroepiandrosterone (DHEA) in LNCaP, with an IC50<1 μM[4].
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| ln Vivo |
Serum concentrations between 0.5 and 1 μM have been previously demonstrated to be produced by the 0.5 mmol/kg/d Abiraterone treatment dosage. In the control group, the growth of xenograft tumors varies greatly; only a small percentage of tumors show vigorous growth, while other tumors grow slowly[4]. The volume of distribution (Vd) and clearance (Cl) after intravenous (5 mg/kg) dosing are determined to be 1.97 L/kg and 31.2 mL/min/kg, respectively. It is determined that 2675 ng*h/mL is the area under the plasma concentration-time curve (AUC0-∞) from time zero to the infinity time point. 0.73 hours is the terminal half-life (t1/2). Abiraterone (ART) is only quantifiable up to two hours after intravenous delivery due to rapid clearance[5].
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| References |
[1]. Attard G, et al. Phase I clinical trial of a selective inhibitor of CYP17, abiraterone acetate, confirms that castration-resistant prostate cancer commonly remains hormone driven. J Clin Oncol. 2008 Oct 1;26(28):4563-71.
[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]. 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. [4]. 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. [5]. Kumar SV, et al. Validated RP-HPLC/UV method for the quantitation of abiraterone in rat plasma and its application to a pharmacokinetic study in rats. Biomed Chromatogr. 2013 Feb;27(2):203-7. [6]. 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 |
| Molecular Formula |
C24H31NO
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|---|---|
| Molecular Weight |
349.51
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| CAS # |
154229-19-3
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| Related CAS # |
Abiraterone acetate;154229-18-2;Abiraterone-d4;2122245-62-7
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| SMILES |
O[C@H]1CC[C@]2(C)[C@@]3([H])CC[C@]4(C)C(C5=CC=CN=C5)=CC[C@@]4([H])[C@]3([H])CC=C2C1
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| InChi Key |
GZOSMCIZMLWJML-VJLLXTKPSA-N
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| InChi Code |
InChI=1S/C24H31NO/c1-23-11-9-18(26)14-17(23)5-6-19-21-8-7-20(16-4-3-13-25-15-16)24(21,2)12-10-22(19)23/h3-5,7,13,15,18-19,21-22,26H,6,8-12,14H2,1-2H3/t18-,19-,21-,22-,23-,24+/m0/s1
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| Chemical Name |
(3S,8R,9S,10R,13S,14S)-10,13-dimethyl-17-(pyridin-3-yl)-2,3,4,7,8,9,10,11,12,13,14,15-dodecahydro-1H-cyclopenta[a]phenanthren-3-ol.
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| Synonyms |
Abiraterone; CB 7598; CB7598; CB-7598; US 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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| Preparing Stock Solutions | 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 |
*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.
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