Bicalutamide-d₄is intended for use as an internal standard for the quantification of bicalutamide by GC- or LC-MS. Bicalutamide is a non-steroidal androgen receptor antagonist that binds the androgen receptor (K_i= 12.5 μM; IC₅₀= 1.2 μM), preventing its activation and subsequent upregulation of androgen responsive genes by androgenic hormones.^1,2Bicalutamide is frequently used to examine the role of androgen receptor inactivation in the proliferation of prostate cancer cells and has served as a molecular template for the design and structural optimization of more selective androgen receptor modulators for androgen therapy.^3,4

1.Freeman, S.N., Mainwaring, W.I.P., and Furr, B.J.A.A possible explanation for the peripheral selectivity of a novel non-steroidal pure antiandrogen, Casodex (ICI 176,334)Br. J. Cancer60(5)664-668(1989) 2.Masiello, D., Cheng, S., Bubley, G.J., et al.Bicalutamide functions as an androgen receptor antagonist by assembly of a transcriptionally inactive receptorThe Journal of Biological Chemisty277(29)26321-26326(2002) 3.Gao, W., Kim, J., and Dalton, J.T.Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligandsPharmaceutical Research23(8)1641-1658(2006) 4.Yin, D., Perera, M.A., Dalton, J.T., et al.Key structural features of nonsteroidal ligands for binding and activation of the androgen receptorMolecular Pharmacology63(1)211-223(2003)