R-Bicalutamide
R-Bicalutimide is an inhibitor of the androgen receptor that exhibits anticancer chemotherapeutic activity. With other anti-androgens, R-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. Optical rotation: [a]20 D= -83.~ – 85.0 (C=1, MeOH)
References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/18957110
| Cas No. |
113299-40-4 |
|---|---|
| Purity |
≥98% |
| Formula |
C18H14F4N2O4S |
| Formula Wt. |
430.37 |
| Chemical Name |
R-N-(4-cyano-3-(trifluoromethyl)phenyl)-3-((4-fluorophenyl)sulfonyl)-2-hydroxy-2-methyl-, (+-)- Propanamide |
| IUPAC Name |
(2R)-N-[4-cyano-3-(trifluoromethyl)phenyl]-3-(4-fluorophenyl)sulfonyl-2-hydroxy-2-methylpropanamide |
| Melting Point |
178-179°C |
| Solubility |
water: 5mg/L |
| Appearance |
White Crystalline 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.
