Bicalutamide Inhibitor CAS No. 90357-06-5

Cat. No.	Name	Size	Price
KI0426	Bicalutamide	50 mg	$192
	Bicalutamide	100 mg	$336
	Bicalutamide	200 mg	$592

Chemical Characteristic

Product Name	Bicalutamide
Synonyms	Casodex, Cosudex, Calutide, Kalumid
CAS No.	90357-06-5
Molecular Weight	430.37
Formula	C₁₈H₁₄F₄N₂O₄S
Chemical Name	N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methyl-propanamide
Smiles	C(=O)(C(CS(=O)(=O)c1ccc(cc1)F)(C)O)Nc1cc(c(cc1)C#N)C(F)(F)F
Chemical Structure

Biological activities

Bicalutamide is a pure androgen receptor (AR) antagonist used in the treatment of prostate cancer and hirsutism. Bicalutamide is binding to the androgen receptor and preventing the activation of the AR and subsequent upregulation of androgen responsive genes by androgenic hormones.^[1] Under dihydrotestosterone (0.1 nM) stimulation, bicalutamide (1 nM, 100 nM and 10 μM) appear to exert a dose-dependent inhibitory action on the growth of LNCaP FGC prostate cancer cell line, with the maximum inhibitory effect achieved by the 10 μM concentration.^[2] Equilibrium-binding affinity of bicalutamide for AR has a median IC50 of 160 nM on LNCaP/AR(cs) prostate cancer cell line. Bicalutamide (10 μM) treatment results in a significant amount of nuclear AR (nuclear/cytoplasmic ratio, 13.8), although less than that observed with the synthetic androgen R1881 (nuclear/cytoplasmic ratio, 29) in LNCaP prostate cancer cell line.^[3] Bicalutamide (100 nM-10 µM) inhibits the proliferation of LNCaP cells, but stimulates proliferation of LNCaP-abl cells. Furthermore, the ability of bicalutamide (100 nM-10 μM) to antagonize the effects of androgen on reporter gene activity is greatly impaired in LNCaP-abl cells generated after long-term androgen ablation.^[4] In castrate mice bearing LNCaP/AR(cs) xenograft tumors, the antitumor activity of bicalutamide (10mg/kg/day) is largely restricted to growth inhibition rather than tumor shrinkage: only 1 of 10 tumors exhibit more than 50% regression and Similar results are obtained in castrate male SCID (severe combined immunodeficiency) mice bearing LNCaP/AR-luc xenograft tumors.^[3] In mice bearing C4-2 prostate cancer xenografts, single bicalutamide (10 mg/kg, administered daily) reduces tumor growth by 79% and the ridaforolimus-bicalutamide combination almost completely abrogates tumor growth by 98%, exhibiting improved and potent antitumor activity.^[5]

References

[1] Furr BJ, et al. The preclinical development of bicalutamide: pharmacodynamics and mechanism of action. Urology. 1996, 47(1A Suppl): 13-25. [2] Boccardo F, et al. 4-OH tamoxifen does not interfere with bicalutamide inhibitory effects on human prostatic cancer cells in vitro. Anticancer Res. 2005, 25(6B): 4277-4280. [3] Clegg NJ, et al. ARN-509: a novel antiandrogen for prostate cancer treatment. Cancer Res. 2012, 72(6): 1494-1503. [4] Culig Z, et al. Switch from antagonist to agonist of the androgen receptor bicalutamide is associated with prostate tumour progression in a new model system. Br J Cancer. 1999, 81(2): 242-251. [5] Squillace RM, et al. Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models. Int J Oncol. 2012, 41(2): 425-32.

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