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Description: Non-steroidal androgen receptor antagonist
Alternative Names: Casodex,ICI 176,334
Chemical Name: N-[4-Cyano-3-(trifluoromethyl)phenyl]-3-[(4-fluorophenyl)sulfonyl]-2-hydroxy-2-methylpropanamide
Purity: ≥99% (HPLC)
Citations (4)
Reviews (1)

Biological Activity for Bicalutamide

Bicalutamide 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.

Licensing Information

Sold for research purposes only under agreement from AstraZeneca

Compound Libraries for Bicalutamide

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.

Technical Data for Bicalutamide

M. Wt 430.37
Formula C18H14F4N2O4S
Storage Store at RT
Purity ≥99% (HPLC)
CAS Number 90357-06-5
PubChem ID 2375
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.

Solubility Data for Bicalutamide

Solvent Max Conc. mg/mL Max Conc. mM
DMSO 43.04 100
ethanol 4.3 10

Preparing Stock Solutions for Bicalutamide

The following data is based on the product molecular weight 430.37. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 2.32 mL 11.62 mL 23.24 mL
5 mM 0.46 mL 2.32 mL 4.65 mL
10 mM 0.23 mL 1.16 mL 2.32 mL
50 mM 0.05 mL 0.23 mL 0.46 mL

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References for Bicalutamide

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

If you know of a relevant reference for Bicalutamide, please let us know.

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Keywords: Bicalutamide, Bicalutamide supplier, Non-steroidal, Androgen, receptor, antagonists, Dihydrotestosterone, Receptors, AstraZeneca, ICI176,334, chemotherapeutics, Casodex, ICI, 176,334, Receptor, 3389, Tocris Bioscience

4 Citations for Bicalutamide

Citations are publications that use Tocris products. Selected citations for Bicalutamide include:

Ivachtchenko et al (2014) Preclinical Development of ONC1-13B, Novel Antiandrogen for Prostate Cancer Treatment. PLoS One 5 133 PMID: 24494031

Olokpa et al (2016) The Androgen Receptor Regulates PPARγ Expression and Activity in Human Prostate Cancer Cells. J Cell Physiol 231 2664 PMID: 26945682

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

Ishizaki et al (2013) Androgen deprivation promotes intratumoral synthesis of dihydrotestosterone from androgen metabolites in prostate cancer. Sci Rep 3 1528 PMID: 23524847

Do you know of a great paper that uses Bicalutamide from Tocris? Please let us know.

Reviews for Bicalutamide

Average Rating: 5 (Based on 1 Review.)

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In vitro culture with c4-2 cells to induce AR reduction.
By Anonymous on 11/03/2019
Assay Type: In Vitro
Species: Human
Cell Line/Tissue: c4-2 cell

in vitro culture with c4-2 cells to induce AR reduction

PMID: 26945682
review image