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Bicalutamide (ICI-176334)
Catalog No.S1190
For research use only.
Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
CAS No. 90357-06-5
Selleck's Bicalutamide (ICI-176334) has been cited by 40 publications
Purity & Quality Control
Choose Selective Androgen Receptor Inhibitors
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Biological Activity
| Description | Bicalutamide (ICI-176334) is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy. | |||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||||
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| In vitro |
Bicalutamide undergoes an antagonist-to-agonist switch, stimulating AR activity. Bicalutamide treatment of LNCaP/AR(cs) cells in absence of the synthetic androgen R1881 results in altered gene expression consistent with its well-documented agonist activity in context of AR overexpression. Bicalutamide induces cell proliferation in a dose-dependent manner, and only partially antagonized the effects of R1881. Bicalutamide treatment also results in a significant amount of nuclear AR, although less than that observed with R1881. Bicalutamide exhibits partial agonist activity as evidenced by induction of DNA binding at AR target genes and incomplete antagonism of the effects of R1881. In absence of R1881, Bicalutamide partially activates VP16-AR–mediated transcription, indicative of AR binding to DNA. In LNCaP/AR-luc cells with a stably integrates AR-driven luciferase reporter construct. In the presence of R1881, Bicalutamide shows only weak partial antagonism of VP16-AR–mediated transcription with an IC50 of 0.35 μM. [1] Micromolar bicalutamide causes a significant dose-dependent reduction in clonogenicity. [2] Dual inhibition of the AR and mTOR signaling pathways provides further benefit with the ridaforolimus-bicalutamide combination producing syner -gistic antiproliferative effects in prostate cancer cells in vitro when compared with each agent alone. [3] |
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| Cell Data |
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| In vivo | Single bicalutamide reduces tumor growth by 79%, at defined submaximal doses. The ridaforolimus-bicalutamide combination exhibits improved and potent antitumor activity, almost completely abrogating tumor growth. The combination is also well tolerated, as evidenced by no significant changes in body weight over the course of treatment. Plasma PSA levels are again tightly linked to tumor growth in the combination-treated mice. [3] |
Protocol (from reference)
| Kinase Assay:[1] |
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| Cell Research:[3] |
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| Animal Research:[3] |
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Solubility (25°C)
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In vitro |
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Chemical Information
| Molecular Weight | 430.37 | ||
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| Formula | C18H14F4N2O4S |
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| CAS No. | 90357-06-5 | ||
| Storage | 3 years | -20°C | powder |
| 2 years | -80°C | in solvent | |
| Smiles | CC(CS(=O)(=O)C1=CC=C(C=C1)F)(C(=O)NC2=CC(=C(C=C2)C#N)C(F)(F)F)O | ||
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Clinical Trial Information
| NCT Number | Recruitment | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|---|
| NCT04573231 | Recruiting | Drug: 18F-DCFPyL | Breast Cancer|HER2-negative Breast Cancer|Metastatic Breast Cancer | University of Wisconsin Madison | May 24 2021 | Phase 2 |
| NCT04443062 | Recruiting | Drug: 177Lu-PSMA-617 | Prostate Cancer | Radboud University|Prostaatkankerstichting|Advanced Accelerator Applications | July 20 2020 | Phase 2 |
| NCT02910050 | Unknown status | Drug: Bicalutamide|Drug: Aromatase Inhibitor | Breast Cancer | Xu fei|Sun Yat-sen University | January 2016 | Phase 2 |
| NCT02614859 | Active not recruiting | Drug: Bicalutamide|Drug: Metformin and Bicalutamide | Cancer of Prostate | Fox Chase Cancer Center|National Cancer Institute (NCI) | December 1 2015 | Phase 2 |
(data from https://clinicaltrials.gov, updated on 2022-01-17)
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