Abiraterone-acetate-CB7630-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEAbiraterone acetateCat. No.: HY-75054CAS No.: 154229-18-2Synonyms: CB7630分式: CHNO分量: 391.55作靶点: Cytochrome P450作通路: Metabolic Enzyme/Protease储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 DMSO :

2、13.3 mg/mL (33.97 mM; Need ultrasonic and warming)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.5540 mL 12.7698 mL 25.5395 mL5 mM 0.5108 mL 2.5540 mL 5.1079 mL10 mM 0.2554 mL 1.2770 mL 2.5540 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 Abiraterone acetate is prepared in 0.1 mL 5% benzy

3、l alcohol and 95% safflower oil solution4.BIOLOGICAL ACTIVITY物活性 Abiraterone acetate种服、有效、选择性和不可逆的 CYP17A1 抑制剂，具有抗雄激素活性。Abiraterone acetate是Abiraterone (CB7598) 的前药形式。IC50 & Target CYP17A1 21/3 Master of Small Molecules 您边的抑制剂师www.MedChemE体外研究 Abiraterone (Abi) acetate is an ester prodrug of the ant

4、icancer agent Abiraterone, which shows IC50 valuesof 15 nM and 2.5 nM for the 17,20-lyase and 17-hydroxylase (CYP17 is a bifunctional enzyme with both 17-hydroxylase and 17,20-lyase activity). Abiraterone inhibits human 17,20-lyase and 17-hydroxylase withIC50 of 27 and 30 nM respectively 1. Signific

5、ant inhibition of proliferation of the AR-positive prostate cancercell lines LNCaP and VCaP with doses of Abiraterone 5 M is confirmed 2. Abiraterone inhibitsrecombinant human 3HSD1 and 3HSD2 activity with competitive Ki values of 2.1 and 8.8 M. 10 MAbiraterone is sufficient to completely block synt

6、hesis of 5-dione and DHT in both cell lines.Treatment withAbiraterone significantly inhibited CRPC progression in the robustly growing subset, effectively putting aceiling on tumor growth over 4 weeks of treatment (P 3.体内研究 Abiraterone (Abi) acetate prolongs survival in castration-resistant prostate

7、 cancer (CRPC). 3H-dehydroepiandrosterone (DHEA) depletion and 4-androstenedione (AD) accumulation are inhibited byAbiraterone in LNCaP, with an IC50 3.PROTOCOLCell Assay 2 LNCaP and VCaP cells are seeded in 96-well plates and grown in CSS-supplemented phenol red-free orFBS-supplemented media for 7

8、days. Cells are treated with Abiraterone (5 M and 10 M) at 24 and 96hours after plating and cell viability is determined on day 7 by adding CellTiter Glo and measuringluminescence 2.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 3Administra

9、tion 3 Male NOD/SCID mice 6 to 8 weeks of age are surgically orchiectomized and implanted with a 5 mg 90-daysustained release DHEA pellet to mimic CRPC with human adrenal physiology. Two days later, 7106LAPC4 cells are injected subcutaneously with Matrigel. Tumor dimensions are measured 2 to 3 times

10、 perweek, and volume is calculated as lengthwidthheight0.52. Once tumors reach 300 mm3, mice arerandomly assigned to vehicle or Abiraterone treatment groups. Mice in the Abiraterone group are treated with5 mL/kg intraperitoneal injections of 0.5 mmol/kg/d (0.1 mL 5% benzyl alcohol and 95% safflower

11、oil solution)and control mice with vehicle only, once daily for 5 days per week over a duration of 4 weeks (n=8 mice pertreatment). Statistical significance between Abiraterone and vehicle treatment groups is assessed by ANOVAbased on a mixed-effect model.MCE has not independently confirmed the accu

12、racy of these methods. They are for reference only.户使本产品发表的科研献 Br J Cancer. 2017 Mar 28;116(7):937-943. Mol Cancer Ther. 2015 Jan;14(1):59-69. Psychology, University of British Columbia. 2017 Aug.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您边的抑制剂师

13、www.MedChemE1. 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

14、forincreasing abiraterone exposure or combining with MDV3100. Cancer Res. 2012 May 1;72(9):2176-82.3. Li R, et al. Abiraterone inhibits 3-hydroxysteroid dehydrogenase: a rationale for increasing drug exposure in castration-resistantprostate 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 ODonnell, et al. Hormonal impact of the 17-hydroxylase/C17,20-lyase inhibitor abiraterone acetate (CB7630) in patients withprostate cancer. British Journal of Cancervolume