Description
Bicalutamide-d
4 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 (K
i = 12.5 μM; IC
50 = 1.2 μM), preventing its activation and subsequent upregulation of androgen responsive genes by androgenic hormones. 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.
Uses
BICALUTAMIDE-D4 is used as an antiandrogen, antineoplastic (hormonal). (94%d4; 5.7%d3, 0.1%d1, no d0
References
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10.1038/bjc.1989.336[2] DAVID MASIELLO. Bicalutamide Functions as an Androgen Receptor Antagonist by Assembly of a Transcriptionally Inactive Receptor*[J]. The Journal of Biological Chemistry, 2002, 28 1: 26321-26326. DOI:
10.1074/jbc.m203310200[3] WENQING GAO J T D Juhyun Kim. Pharmacokinetics and pharmacodynamics of nonsteroidal androgen receptor ligands.[J]. Pharmaceutical Research, 2006, 23 8: 1641-1658. DOI:
10.1007/s11095-006-9024-3[4] DONGHUA YIN. Key structural features of nonsteroidal ligands for binding and activation of the androgen receptor.[J]. Molecular Pharmacology, 2003, 63 1: 211-223. DOI:
10.1124/mol.63.1.211
