Home Endocrinology & Hormones Androgen Receptor antagonist - Autophagy activator Bicalutamide For research use only.

Bicalutamide

Synonyms: ICI-176334

Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.

Bicalutamide Chemical Structure

Bicalutamide Chemical Structure

CAS No. 90357-06-5

Purity & Quality Control

Bicalutamide Related Products

Signaling Pathway

Androgen Receptor Signaling Pathways

Androgen Receptor Signaling Pathway

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human MDA-MB-453 cells Function assay Displacement of [3H]R1881 from AR in human MDA-MB-453 cells, EC50=31 nM 23713567
LNCaP cells Function assay Inhibition of [3H]-DHT binding to T877A androgen receptor of LNCaP cells, Ki=35 nM 15603960
Freestyle293F cells Function assay Inhibition of wild type Androgen receptor (unknown origin) expressed in Freestyle293F cells, IC50=0.054 μM 23199477
HEK293 cells Function assay 3 h Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs, IC50=54 nM 22391033
MDA453 cells Function assay Displacement of [3H]DHT from human androgen receptor in MDA453 cells, Ki=64 nM 18291644
human MDA-MB-453 cells Function assay Displacement of [3H]DHT from AR in human MDA-MB-453 cells, IC50=64 nM 20584610
COS1 cells Function assay Antagonist activity against pSG5-tagged human androgen receptor expressed in COS1 cells assessed as reduction in receptor-mediated transcriptional activity by AR-regulated rat probasin promoter fragment driven firefly luciferase reporter assay, IC50=0.0869 μM 25646649
HeLa cells Function assay Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay, IC50=0.14 μM 17804229
CV1 cells Function assay Binding affinity to human androgen receptor expressed in CV1 cells, Ki=0.151 μM 17257838
monkey COS7 cells Function assay Binding affinity to human androgen receptor expressed in monkey COS7 cells by whole cell binding assay, Ki=0.151 μM 18442912
COS7 cells Function assay Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay, EC50=0.18 μM 22094279
CHO-K1 cells Function assay 2 h Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting, IC50=0.2 μM 20381361
human HT-3 cell Growth inhibition assay Inhibition of human HT-3 cell growth in a cell viability assay, IC50=0.73134 μM SANGER
human LNCAP cells Proliferation assay 3 days Antiproliferative activity against human LNCAP cells after 3 days, IC50=0.7327 μM 26046313
human PC3 cells Function assay Displacement of [3H]R1881 from androgen receptor in human PC3 cells, EC50=4.3 μM 25591066
human 22Rv1 cells Function assay 3 days Antagonist activity at androgen receptor H874Y mutant (unknown origin) expressed in human 22Rv1 cells assessed as inhibition of DHT-induced cell growth after 3 days by WST-8 assay, IC50=4.6 μM 24900588
human CCF-STTG1 cell Growth inhibition assay Inhibition of human CCF-STTG1 cell growth in a cell viability assay， IC50=4.92929 μM SANGER
human SCC-25 cell Growth inhibition assay Inhibition of human SCC-25 cell growth in a cell viability assay, IC50=6.08656 μM SANGER
human MKN45 cell Growth inhibition assay Inhibition of human MKN45 cell growth in a cell viability assay, IC50=6.9605 μM SANGER
human ES5 cell Growth inhibition assay Inhibition of human ES5 cell growth in a cell viability assay, IC50=8.61154 μM SANGER
human SK-MEL-3 cell Growth inhibition assay Inhibition of human SK-MEL-3 cell growth in a cell viability assay, IC50=10.0964 μM SANGER
human PC-3 cell Growth inhibition assay Inhibition of human PC-3 cell growth in a cell viability assay, IC50=10.2791 μM SANGER
human NOS-1 cell Growth inhibition assay Inhibition of human NOS-1 cell growth in a cell viability assay, IC50=11.2917 μM SANGER
human LB1047-RCC cell Growth inhibition assay Inhibition of human LB1047-RCC cell growth in a cell viability assay, IC50=12.253 μM SANGER
human CAMA-1 cell Growth inhibition assay Inhibition of human CAMA-1 cell growth in a cell viability assay, IC50=12.3926 μM SANGER
human SAS cell Growth inhibition assay Inhibition of human SAS cell growth in a cell viability assay, IC50=13.3081 μM SANGER
human NCI-H2228 cell Growth inhibition assay Inhibition of human NCI-H2228 cell growth in a cell viability assay, IC50=13.7531 μM SANGER
human NCI-H187 cell Growth inhibition assay Inhibition of human NCI-H187 cell growth in a cell viability assay, IC50=16.6616 μM SANGER
human BFTC-905 cell Growth inhibition assay Inhibition of human BFTC-905 cell growth in a cell viability assay, IC50=17.4857 μM SANGER
human G-361 cell Growth inhibition assay Inhibition of human G-361 cell growth in a cell viability assay, IC50=17.826 μM SANGER
human DU145 cells Cytotoxic assay 72 h Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay, IC50=18 μM SANGER
human SW780 cell Growth inhibition assay Inhibition of human SW780 cell growth in a cell viability assay SANGER
human BB49-HNC cell Growth inhibition assay Inhibition of human BB49-HNC cell growth in a cell viability assay, IC50=18.9532 μM SANGER
human KALS-1 cell Growth inhibition assay Inhibition of human KALS-1 cell growth in a cell viability assay, IC50=19.6635 μM SANGER
human AU565 cell Growth inhibition assay Inhibition of human AU565 cell growth in a cell viability assay, IC50=19.7402 μM SANGER
human NCI-H2087 cell Growth inhibition assay Inhibition of human NCI-H2087 cell growth in a cell viability assay, IC50=21.0591 μM SANGER
human RVH-421 cell Growth inhibition assay Inhibition of human RVH-421 cell growth in a cell viability assay, IC50=21.5795 μM SANGER
human SK-CO-1 cell Growth inhibition assay Inhibition of human SK-CO-1 cell growth in a cell viability assay, IC50=21.8872 μM SANGER
human KU-19-19 cell Growth inhibition assay Inhibition of human KU-19-19 cell growth in a cell viability assay, IC50=22.0242 μM SANGER
human NB6 cell Growth inhibition assay Inhibition of human NB6 cell growth in a cell viability assay, IC50=22.9135 μM SANGER
human RO82-W-1 cell Growth inhibition assay Inhibition of human RO82-W-1 cell growth in a cell viability assay, IC50=23.1318 μM SANGER
human LNCAP cells Cytotoxic assay 2 days Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method, IC50=23.79 μM 23727044
human CTB-1 cell Growth inhibition assay Inhibition of human CTB-1 cell growth in a cell viability assay, IC50=24.5536 μM SANGER
human SW48 cell Growth inhibition assay Inhibition of human SW48 cell growth in a cell viability assay, IC50=24.6546 μM SANGER
human TCCSUP cell Growth inhibition assay Inhibition of human TCCSUP cell growth in a cell viability assay, IC50=24.7232 μM SANGER
human DK-MG cell Growth inhibition assay Inhibition of human DK-MG cell growth in a cell viability assay, IC50=24.8917 μM SANGER
human ST486 cell Growth inhibition assay Inhibition of human ST486 cell growth in a cell viability assay, IC50=25.7464 μM SANGER
human H4 cell Growth inhibition assay Inhibition of human H4 cell growth in a cell viability assay, IC50=26.9458 μM SANGER
human SBC-1 cell Growth inhibition assay Inhibition of human SBC-1 cell growth in a cell viability assay, IC50=28.3507 μM SANGER
human CAS-1 cell Growth inhibition assay Inhibition of human CAS-1 cell growth in a cell viability assay, IC50=28.6294 μM SANGER
human OAW-42 cell Growth inhibition assay Inhibition of human OAW-42 cell growth in a cell viability assay, IC50=28.7195 μM SANGER
human HCC1954 cell Growth inhibition assay Inhibition of human HCC1954 cell growth in a cell viability assay, IC50=28.7525 μM SANGER
human MDA-MB-453 cell Growth inhibition assay Inhibition of human MDA-MB-453 cell growth in a cell viability assay, IC50=29.907 μM SANGER
human MCF7 cell Growth inhibition assay Inhibition of human MCF7 cell growth in a cell viability assay, IC50=39.301 μM SANGER
human PC3 cells Function assay 100　μM 48 h Inhibition of actin based pseudopodia formation in androgen-dependent human PC3 cells at 100 uM after 48 hrs by DAPI staining based fluorescence microscopy assay 22672984
human PC3 cells Function assay 0.1-1 μM Agonist activity at androgen receptor W741C mutant expressed in human PC3 cells assessed as stimulation of receptor transactivation at 0.1 to 1 uM by luciferase reporter gene assay 22175694
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Biological Activity

Description Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line. Bicalutamide promotes autophagy.
Targets
Androgen Receptor [1]
(LNCaP/AR(cs) cells)
0.16 μM
In vitro
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]
Kinase Assay Whole-cell competitive binding assays
Whole-cell competitive binding assays are performed in LNCaP/AR(codon-switch) (LNCaP/AR(cs)) (harbors a mixture of exogenous wild-type AR and endogenous mutant AR (T877A)) and cells propagated in Iscove's or RPMI media supplemented with 10% fetal bovine serum, or during the assay with 10% charcoal-stripped, dextran-treated fetal bovine serum (CSS). Cells are pre-incubated with 18F-FDHT, increasing concentrations (1pM to 1μM) of cold Bicalutamide are added, and the assay is performed to measure specific uptake of 18F-FDHT (4). IC50 values are determined using a one site binding model with least squares curve fitting and R2 > 0.99.
Cell Research Cell lines C4-2 cell
Concentrations 0-1 μM
Incubation Time 72 hours
Method Exponentially growing C4-2 cells are plated into two 96-well plates and incubated overnight at 37 ˚C. Twenty-four hours later one plate is aspirated and stored at -80 ˚C and the other treated with 10-fold serial concentrations of ridaforolimus (1000 nM to 0.0001 nM) or vehicle (ethanol). Following 72 hours culture at 37 ˚C, the plates are assessed simultaneously for cell growth using the Cy qUANT Cell Proliferation Assay kit. Bicalutamide and Ridaforolimus combination proliferation assays are performed similarly except cell growth is determined as the change in cell number between vehicle control and compound treated cells after 72 hours in culture.
Experimental Result Images Methods Biomarkers Images PMID
Western blot Cytosolic AR / Nuclear AR 30833616
Growth inhibition assay Cell viability 27994514
In Vivo
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]
Animal Research Animal Models Male nude mice bearing C4-2 cells
Dosages 10 mg/kg
Administration Administered via p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06222593 Not yet recruiting
Carcinoma Renal Cell
State University of New York at Buffalo
 June 1 2024 Phase 1|Phase 2
NCT04573231 Recruiting
Breast Cancer|HER2-negative Breast Cancer|Metastatic Breast Cancer
University of Wisconsin Madison
 May 24 2021 Phase 2
NCT04443062 Recruiting
Prostate Cancer
Radboud University Medical Center|Prostaatkankerstichting|Advanced Accelerator Applications
 July 20 2020 Phase 2
NCT02910050 Unknown status
Breast Cancer
Xu fei|Sun Yat-sen University
 January 2016 Phase 2

Chemical Information & Solubility

Molecular Weight 430.37 Formula

C18H14F4N2O4S
CAS No. 90357-06-5 SDF Download Bicalutamide SDF
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
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 86 mg/mL ( (199.82 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 7 mg/mL

Water : Insoluble


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