RU 56279 is an androgen receptor ( AR ) antagonist with strong and systemic anti-androgenic activity. RU 56279 is also a common, potent and long-lasting anti-androgen metabolite of RU 56187 and RU 58841 in vivo. RU 56279 can be used as an AR ligand to construct an AR-targeted prodrug system for the study of AR-positive tumor cells [1] [2].
References:
[1]. Cousty-Berlin D, et al. Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: relation of their systemic activity to the formation of a common metabolite. J Steroid Biochem Mol Biol. 1994 Oct;51(1-2):47-55.
[2]. Cogan PS, Koch TH. Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate. J Med Chem. 2003 Nov 20;46(24):5258-70.
References:
[1]. Cousty-Berlin D, et al. Preliminary pharmacokinetics and metabolism of novel non-steroidal antiandrogens in the rat: relation of their systemic activity to the formation of a common metabolite. J Steroid Biochem Mol Biol. 1994 Oct;51(1-2):47-55.
[2]. Cogan PS, Koch TH. Rational design and synthesis of androgen receptor-targeted nonsteroidal anti-androgen ligands for the tumor-specific delivery of a doxorubicin-formaldehyde conjugate. J Med Chem. 2003 Nov 20;46(24):5258-70.