Abiraterone Inhibitor CAS No. 154229-19-3

Cat. No.	Name	Size	Price
KI0377	Abiraterone	10 mg	$150
	Abiraterone	50 mg	$270
	Abiraterone	100 mg	$400

Chemical Characteristic

Product Name	Abiraterone
Synonyms	CB-7598
CAS No.	154229-19-3
Molecular Weight	349.51
Formula	C₂₄H₃₁NO
Chemical Name	17-?(3-?pyridinyl)?-?(3?)?-androsta-?5,?16-?dien-?3-?ol
Smiles	[C@@H]1(CC[C@]2(C(=CC[C@H]3[C@@H]4CC=C([C@@]4(C)CC[C@H]23)c2cnccc2)C1)C)O
Chemical Structure

Biological activities

Abiraterone is an oral, potent, selective, and irreversible inhibitor of 17α-hydroxylase-C_{17, 20-lyase (CYP17). Abiraterone is 10- to 30-fold more potent than the nonselective inhibitor ketoconazole.^[1] Abiraterone is a potent inhibitor of the CYP17 enzyme with a apparent inhibition constants (Ki_{app) of <1 nM. ^[2] Abiraterone potently blocks cytochrome CYP17, a critical enzyme in testosterone synthesis, thereby blocking androgen synthesis by the adrenal glands, testes and within the prostate tumor. ^[3] In vitro, abiraterone inhibits adrenocorticotropic hormone (ACTH) -mediated stimulation of adrenal cells. In male WHT mice, administration of the acetylated prodrug form of abiraterone causes a reduction in androgen-dependent organs including the prostate, seminal vesicles, testes and kidneys, and also leads to a marked dose-dependent decrease in circulating testosterone levels. ^[4] Abiraterone potently inhibits the C_{17, 20-lyase with an IC50 of 5.8 nM in rat testis microsomes. ^[5] Abiraterone inhibits CYP17 in human and rat testicular microsomes and in E. coli cells with IC50s of 73, 220 and 54 nM, respectively. ^[6]}}}

References

[1] Reid AH, et al. Significant and sustained antitumor activity in post-docetaxel, castration-resistant prostate cancer with the CYP17 inhibitor abiraterone acetate. J Clin Oncol. 2010, 28(9): 1489-1495. [2] Martins V, et al. A validated liquid chromatographic-tandem mass spectroscopy method for the quantification of abiraterone acetate and abiraterone in human plasma. J Chromatogr B Analyt Technol Biomed Life Sci. 2006, 843(2): 262-267. [3] Parker C, et al. Abiraterone and increased survival in metastatic prostate cancer. N Engl J Med. 2011, 365(8): 767. [4] Pezaro CJ, et al. Abiraterone acetate: redefining hormone treatment for advanced prostate cancer. Drug Discov Today. 2012, 17(5-6): 221-226. [5] Haidar S, et al. Effects of novel 17alpha-hydroxylase/C_{17, 20-lyase (P450 17, CYP 17) inhibitors on androgen biosynthesis in vitro and in vivo. Effects of novel 17alpha-hydroxylase/C_{17, 20-lyase (P45017, CYP17) inhibitors on androgen biosynthesis in vitro and in vivo. J Steroid Biochem Mol Biol. 2003, 84(5): 555-562.}} [6] Duc I, et al. In vitro and in vivo models for the evaluation of potent inhibitors of male rat 17alpha-hydroxylase/C_{17, 20-lyase. J Steroid Biochem Mol Biol. 2003, 84(5): 537-542.}

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