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Submit ReviewBicalutamide is an orally active non-steroidal androgen receptor antagonist (IC50 = 190 nM). Displays peripheral selectivity and does not effect serum levels of LH and testosterone. Exhibits potent anticancer activity in vivo.
Sold for research purposes only under agreement from AstraZeneca
Bicalutamide is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen FDA-Approved Drugs. Find out more about compound libraries available from Tocris.
M. Wt | 430.37 |
Formula | C18H14F4N2O4S |
Storage | Store at RT |
Purity | ≥99% (HPLC) |
CAS Number | 90357-06-5 |
PubChem ID | 2375 |
InChI Key | LKJPYSCBVHEWIU-UHFFFAOYSA-N |
Smiles | O=C(C(O)(C)CS(C2=CC=C(F)C=C2)(=O)=O)NC1=CC(C(F)(F)F)=C(C#N)C=C1 |
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
References are publications that support the biological activity of the product.
Furr et al (1987) ICI 176,334: a novel non-steroidal, peripherally selective antiandrogen. J.Endocrinol. 113 R7 PMID: 3625091
Tucker et al (1988) Nonsteroidal antiandrogens. Synthesis and structure-activity relationships of 3-substituted derivatives of 2-hydroxypropionanilides. J.Med.Chem. 31 954 PMID: 3361581
Furr and Tucker (1996) The preclinical development of bicalutamide: pharmacodynamics and mechanism of action. Urology 47 13 PMID: 8560673
Keywords: Bicalutamide, Bicalutamide supplier, Non-steroidal, Androgen, receptor, antagonists, Dihydrotestosterone, Receptors, AstraZeneca, ICI176,334, chemotherapeutics, Casodex, ICI, 176,334, Receptor, 3389, Tocris Bioscience
Citations are publications that use Tocris products. Selected citations for Bicalutamide include:
Gambara et al (2015) TLR3 engagement induces IRF-3-dependent apoptosis in androgen-sensitive prostate cancer cells and inhibits tumour growth in vivo. J Cell Mol Med 19 327 PMID: 25444175
Ivachtchenko et al (2014) Preclinical Development of ONC1-13B, Novel Antiandrogen for Prostate Cancer Treatment. PLoS One 5 133 PMID: 24494031
Ishizaki et al (2013) Androgen deprivation promotes intratumoral synthesis of dihydrotestosterone from androgen metabolites in prostate cancer. Sci Rep 3 1528 PMID: 23524847
Olokpa et al (2016) The Androgen Receptor Regulates PPARγ Expression and Activity in Human Prostate Cancer Cells. J Cell Physiol 231 2664 PMID: 26945682
Average Rating: 5 (Based on 1 Review.)
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in vitro culture with c4-2 cells to induce AR reduction