Bicalutamide
Bicalutimide is an inhibitor of the androgen receptor that exhibits anticancer chemotherapeutic activity. With other anti-androgens, bicalutimide decreases levels of Bcl-2, Bcl-XL, caspase-3, and PARP, induces apoptosis, and inhibits cell growth of prostate cancer cells. In similar animal models, this compound decreases plasma PSA levels and suppresses tumor growth. Bicalutamide binds the androgen receptor in two sites, distorting coactivator binding and inhibiting transcription.
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18844090
| Cas No. |
90357-06-5 |
|---|---|
| Purity |
≥98% |
| Formula |
C18H14F4N2O4S |
| Formula Wt. |
430.37 |
| Chemical Name |
N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-, (+-)- Propanamide |
| IUPAC Name |
N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide |
| Synonym |
Casodex |
| Melting Point |
191-193°C |
| Solubility |
Soluble in acetone, DMSO (86mg/m), ethanol (7 mg/mL) or THF. Slightly soluble in chloroform or ether. Practically insoluble in water. |
| Appearance |
White Crystal Powder |
Squillace RM, Miller D, Wardwell SD, et al. Synergistic activity of the mTOR inhibitor ridaforolimus and the antiandrogen bicalutamide in prostate cancer models. Int J Oncol. 2012 Aug;41(2):425-32. PMID: 22614157.
Yan J, Xie B, Capodice JL, et al. Zyflamend inhibits the expression and function of androgen receptor and acts synergistically with bicalutimide to inhibit prostate cancer cell growth. Prostate. 2012 Feb;72(3):244-52. PMID: 21656835.
De Amicis F, Thirugnansampanthan J, Cui Y, et al. Androgen receptor overexpression induces tamoxifen resistance in human breast cancer cells. Breast Cancer Res Treat. 2010 May;121(1):1-11. PMID: 19533338.
