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Bicalutamide-d4 is 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 (Ki = 12.5 μM; IC50 = 1.2 μM), preventing its activation and subsequent upregulation of androgen responsive genes by androgenic hormones.1,2 Bicalutamide 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)

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