Cat. No.: HY-14249

Bicalutamide

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Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer.

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Pureté: 99.92%
CAS No.: 90357-06-5
Formule: C₁₈H₁₄F₄N₂O₄S
Masse moléculaire:430.37

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Bicalutamide Chemical Structure

CAS No.: 90357-06-5

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Description

Bicalutamide is an orally active non-steroidal androgen receptor (AR) antagonist. Bicalutamide can be used for the research of prostate cancer^[1].

IC₅₀ & Target

Androgen receptor^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
Cancer cell lines	IC₅₀	725 nM Compound: 1	Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation Inhibition of androgen dependent human prostate cancer cell MDA-MB-PCa2b proliferation	[PMID: 15603938]
Cancer cell lines	IC₅₀	400 nM Compound: 1	Inhibition of T877A androgen receptor of human prostate cancer cells in reporter gene assay Inhibition of T877A androgen receptor of human prostate cancer cells in reporter gene assay	[PMID: 15603960]
Cancer cell lines	IC₅₀	18 μM Compound: 5, casodex	Growth inhibition of human castration-resistant prostate cancer cells Growth inhibition of human castration-resistant prostate cancer cells	[PMID: 25591066]
CHO-K1	IC₅₀	200 nM Compound: 3	Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells Displacement of [3H]mibolerone from androgen receptor expressed in CHOK1 cells	[PMID: 17064916]
CHO-K1	IC₅₀	200 nM Compound: 3	Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells Displacement of [3H]mibolerone from human androgen receptor expressed in CHOK1 cells	[PMID: 17804229]
CHO-K1	IC₅₀	200 nM Compound: 3	Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting Displacement of [3H]mibolerone from human AR expressed in CHO-K1 cells after 2 hrs by scintillation counting	[PMID: 20381361]
COS-1	IC₅₀	86.9 nM Compound: Bic	Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition Displacement of [3H]R1881 from pSG5-tagged human androgen receptor expressed in COS1 cells assessed as relative binding inhibition	[PMID: 25646649]
COS-1	IC₅₀	8.69 x 10^-8 M Compound: Bic	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 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	[PMID: 25646649]
COS-1	IC₅₀	8.69 x 10^-2 μM Compound: Bic	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 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	[PMID: 25646649]
COS-7	IC₅₀	0.85 μM Compound: bicalutamide	Inhibition of rat AR-mediated reporter gene expression in COS7 cells Inhibition of rat AR-mediated reporter gene expression in COS7 cells	[PMID: 16603353]
COS-7	EC₅₀	>10 μM Compound: Bicalutamide	Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human androgen receptor expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	EC₅₀	>10 μM Compound: Bicalutamide	Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	EC₅₀	0.18 μM Compound: Bicalutamide	Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay Agonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	IC₅₀	>10 μM Compound: Bicalutamide	Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay Antagonist activity at human androgen receptor W741C mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	IC₅₀	0.33 μM Compound: Bicalutamide	Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay Antagonist activity at human androgen receptor expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	IC₅₀	0.47 μM Compound: Bicalutamide	Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay Antagonist activity at human androgen receptor T877A mutant expressed in COS7 cells assessed as inhibition of DHT-induced luciferase activity after 24 hrs by reporter gene assay	[PMID: 22094279]
COS-7	EC₅₀	>10 μM Compound: Bicalutamide	Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay Agonist activity at androgen receptor expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22391033]
COS-7	EC₅₀	>10 μM Compound: Bicalutamide	Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay Agonist activity at androgen receptor T877A mutant expressed in Cos7 cells after 24 hrs by luciferase reporter gene assay	[PMID: 22391033]
COS-7	IC₅₀	0.33 μM Compound: Bicalutamide	Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay Antagonist activity at androgen receptor expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay	[PMID: 22391033]
COS-7	IC₅₀	0.47 μM Compound: Bicalutamide	Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay Antagonist activity at androgen receptor T877A mutant expressed in Cos7 cells assessed as inhibition of dihydrotestosterone-induced luciferase activity after 24 hrs by reporter gene assay	[PMID: 22391033]
COS-7	IC₅₀	0.33 μM Compound: Bicalutamide	Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay Antagonist activity at wild type Androgen receptor (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay	[PMID: 23199477]
COS-7	IC₅₀	0.47 μM Compound: Bicalutamide	Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay Antagonist activity at Androgen receptor T877A mutant (unknown origin) expressed in human Cos-7 cells co-expressing pGL3-MMTV-luc vector assessed as luciferase activity by reporter gene assay	[PMID: 23199477]
CV-1	EC₅₀	157 nM Compound: Bicalutamide	In vitro antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cells In vitro antagonistic activity against human androgen receptor (hAR) expressed in CV-1 cells	[PMID: 10230628]
CV-1	IC₅₀	>10 nM Compound: Bicalutamide	In vitro agonistic activity against human androgen receptor (hAR) expressed in CV-1 cells; not active In vitro agonistic activity against human androgen receptor (hAR) expressed in CV-1 cells; not active	[PMID: 10230628]
CV-1	IC₅₀	338 nM Compound: 2 (Bicalutamide)	Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells Inhibitory concentration against human androgen receptor (AR) dependent transcriptional activity in co-transfected mammalian CV-1 cells	[PMID: 10743937]
CV-1	IC₅₀	162 nM Compound: bicalutamide	Antagonist activity at human androgen receptor expressed in CV1 cells Antagonist activity at human androgen receptor expressed in CV1 cells	[PMID: 17257838]
CV-1	IC₅₀	162 nM Compound: bicalutamide	Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay Antagonist activity at human androgen receptor in CV1 cells by transcriptional activation assay	[PMID: 18400499]
CV-1	IC₅₀	162 nM Compound: Bicalutamide	Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay Antagonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay	[PMID: 18442912]
CV-1	EC₅₀	>10000 nM Compound: Bicalutamide	Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay Agonist activity at human androgen receptor african green monkey CV1 cells by cotransfection assay	[PMID: 18442912]
CV-1	IC₅₀	0.3 μM Compound: Casodex	Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in human CV1 cells assessed as inhibition of receptor-mediated transactivation by MMTV-luciferase reporter gene assay	[PMID: 20826091]
CV-1	IC₅₀	157 nM Compound: 3	Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells. Antagonistic activity against human androgen receptor (hAR) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	1819 nM Compound: 3	Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells. Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells.	[PMID: 9484511]
CV-1	IC₅₀	157 nM Compound: 3	Antagonistic activity (IC50) against human androgen receptor (hAR) in co-transfected CV-1 cell Antagonistic activity (IC50) against human androgen receptor (hAR) in co-transfected CV-1 cell	[PMID: 9871534]
CWR22R	IC₅₀	4.6 μM Compound: 4	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 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	[PMID: 24900588]
CWR22R	GI₅₀	3.81 μM Compound: Casodex	Growth inhibition of human CWR22Rv1 cells by MTT assay Growth inhibition of human CWR22Rv1 cells by MTT assay	[PMID: 25634130]
CWR22R	IC₅₀	46.25 μM Compound: Bicalutamide	Antiproliferative activity against human 22Rv1 cells after 96 hrs by Oncotest monolayer assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by Oncotest monolayer assay	[PMID: 26965862]
CWR22R	IC₅₀	48.49 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human 22Rv1 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
CWR22R	IC₅₀	49.577 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
CWR22R	IC₅₀	49.58 μM Compound: RS-Bicalutamide	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
CWR22R	IC₅₀	49.6 μM Compound: 1	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
CWR22R	IC₅₀	46.25 μM Compound: Bicalutamide	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability	[PMID: 33513386]
DU-145	IC₅₀	64 μM Compound: Casodex	Cytotoxicity against human androgen-independent DU145 cells by MTT assay Cytotoxicity against human androgen-independent DU145 cells by MTT assay	[PMID: 22326399]
DU-145	IC₅₀	18 μM Compound: Bicalutamide	Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against ERalpha-deficient human DU145 cells expressing ERbeta assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23786452]
DU-145	IC₅₀	46.031 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human DU145 cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
DU-145	IC₅₀	49.2 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
DU-145	IC₅₀	49.2 μM Compound: RS-Bicalutamide	Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human DU145 cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
DU-145	IC₅₀	49.2 μM Compound: 1	Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human DU145 cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
DU-145	IC₅₀	45.41 μM Compound: Bicalutamide	Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability Antiproliferative activity against human DU-145 cells assessed as reduction in cell viability	[PMID: 33513386]
HEK293	IC₅₀	0.054 μM Compound: Bicalutamide	Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor expressed in HEK293 derived FreeStyle293F cells after 3 hrs	[PMID: 22094279]
HEK293	IC₅₀	0.12 μM Compound: Bicalutamide	Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs Displacement of [17-alpha-methyl-3H]-mibolerone from human androgen receptor T877A mutant expressed in HEK293 derived FreeStyle293F cells after 3 hrs	[PMID: 22094279]
HEK293	IC₅₀	0.054 μM Compound: Bicalutamide	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor expressed in HEK293 cells after 3 hrs	[PMID: 22391033]
HEK293	IC₅₀	0.12 μM Compound: Bicalutamide	Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs Displacement of [17-alpha-methyl-3H]mibolerone from androgen receptor T877A mutant expressed in HEK293 cells after 3 hrs	[PMID: 22391033]
HeLa	IC₅₀	140 nM Compound: 3	Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay Antagonist activity at androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone-induced transcriptional activity by reporter gene assay	[PMID: 17064916]
HeLa	IC₅₀	140 nM Compound: 3	Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay Antagonist activity at human androgen receptor expressed in HeLa cells assessed as inhibition of dihydrotestosterone induced transcriptional activity by reporter gene assay	[PMID: 17804229]
HeLa	IC₅₀	200 nM Compound: 3	Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay Antagonist activity at human AR expressed in human HeLa cells co-transfected with MMTV-Luc-Hyg after 48 hrs by transient-luciferase reporter gene assay	[PMID: 21050768]
LNCaP	IC₅₀	0.4 μM Compound: 1	In vitro antagonistic activity against mutant androgen receptor of LNCap cells In vitro antagonistic activity against mutant androgen receptor of LNCap cells	[PMID: 15546739]
LNCaP	IC₅₀	400 nM Compound: 1	Inhibition of mutant T877A Androgen receptor in human LNCaP cells Inhibition of mutant T877A Androgen receptor in human LNCaP cells	[PMID: 15603938]
LNCaP	IC₅₀	940 nM Compound: Casodex	Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells Displacement of [3H]R-1881 from Androgen receptor of LNCaP cells	[PMID: 15828836]
LNCaP	IC₅₀	1 μM Compound: 1	Inhibition of prostate specific antigen expression in human LNCAP cells in presence of fetal bovine serum Inhibition of prostate specific antigen expression in human LNCAP cells in presence of fetal bovine serum	[PMID: 20218717]
LNCaP	IC₅₀	550 nM Compound: 3	Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days Antagonist activity at AR in bicalutamide-resistant human LNCAP cells assessed as effect on cell proliferation after 6 days	[PMID: 20381361]
LNCaP	IC₅₀	400 nM Compound: 5	Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay Antagonist activity at wild type human AR expressed in human LNCAP cells by transactivation assay	[PMID: 20584610]
LNCaP	IC₅₀	600 nM Compound: 3	Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days Antagonist activity at AR in human bicalutamide-resistant LNCAP cells assessed as inhibition of cell proliferation after 6 days	[PMID: 21050768]
LNCaP	IC₅₀	1.71 μM Compound: Casodex	Cytotoxicity against human androgen-dependent LNCAP cells by MTT assay Cytotoxicity against human androgen-dependent LNCAP cells by MTT assay	[PMID: 22326399]
LNCaP	IC₅₀	74 μM Compound: (R,S)Bicalutamide	Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay Cytotoxicity against androgen-dependent human LNCAP cells after 72 hrs by SRB assay	[PMID: 22672984]
LNCaP	IC₅₀	>100 μM Compound: Casodex	Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days Inhibition of BF3 site of androgen receptor in enzalutamide-resistant human LNCAP cells assessed as reduction in PSA level after 3 days	[PMID: 23301637]
LNCaP	EC₅₀	1.4 μM Compound: 2	Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis Displacement of [3H]R1881 from AR in human LNCaP cells after 2 hrs by scintillation counting analysis	[PMID: 23713567]
LNCaP	IC₅₀	0.27 μM Compound: Bicalutamide	Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay Inhibition of androgen receptor in human LNCAP cells after 1 day by luciferase reporter gene assay	[PMID: 23727044]
LNCaP	IC₅₀	23.79 μM Compound: Bicalutamide	Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method Cytotoxicity against human LNCAP cells assessed as cell viability after 2 days by cell counting method	[PMID: 23727044]
LNCaP	IC₅₀	0.94 μM Compound: 4	Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by WST-8 assay Antagonist activity at androgen receptor T877A mutant (unknown origin) expressed in human LNCAP cells assessed as inhibition of DHT-induced cell growth after 6 days by WST-8 assay	[PMID: 24900588]
LNCaP	IC₅₀	30 μM Compound: 2	Growth inhibition of human LNCAP cells Growth inhibition of human LNCAP cells	[PMID: 25301770]
LNCaP	EC₅₀	971 nM Compound: 5, casodex	Displacement of [3H]R1881 from androgen receptor in human LNCAP cells Displacement of [3H]R1881 from androgen receptor in human LNCAP cells	[PMID: 25591066]
LNCaP	GI₅₀	2.61 μM Compound: Casodex	Growth inhibition of human LNCAP cells by MTT assay Growth inhibition of human LNCAP cells by MTT assay	[PMID: 25634130]
LNCaP	IC₅₀	732.7 nM Compound: 2	Antiproliferative activity against human LNCAP cells after 3 days Antiproliferative activity against human LNCAP cells after 3 days	[PMID: 26046313]
LNCaP	IC₅₀	2.38 μM Compound: BIC	Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 4 days by MTT assay in presence of DHT and E2 Cytotoxicity against human LNCAP cells assessed as reduction in cell viability after 4 days by MTT assay in presence of DHT and E2	[PMID: 26780832]
LNCaP	IC₅₀	45.269 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
LNCaP	IC₅₀	47.266 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human LNCAP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
LNCaP	IC₅₀	45.27 μM Compound: RS-Bicalutamide	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
LNCaP	IC₅₀	45.3 μM Compound: 1	Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
LNCaP	IC₅₀	1.5 μM Compound: Bicalutamide	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 33421712]
LNCaP	IC₅₀	45.2 μM Compound: Bicalutamide	Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability Antiproliferative activity against human LNCaP cells assessed as reduction in cell viability	[PMID: 33513386]
LNCaP	IC₅₀	160 nM Compound: 55	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 35786895]
MDA-MB-435	IC₅₀	173 nM Compound: 5	Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay Antagonist activity at human wild type AR expressed in human MDA-MB-435 cells by transactivation assay	[PMID: 20584610]
PC-3	IC₅₀	77 μM Compound: Casodex	Cytotoxicity against human androgen-independent PC3 cells by MTT assay Cytotoxicity against human androgen-independent PC3 cells by MTT assay	[PMID: 22326399]
PC-3	IC₅₀	76.4 μM Compound: (R,S)Bicalutamide	Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay Cytotoxicity against androgen-independent human PC3 cells after 72 hrs by SRB assay	[PMID: 22672984]
PC-3	IC₅₀	>10 μM Compound: 4	Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST-8 assay Cytotoxicity against human PC3 cells assessed as growth inhibition after 3 days by WST-8 assay	[PMID: 24900588]
PC-3	IC₅₀	58 μM Compound: 2	Growth inhibition of human PC3 cells Growth inhibition of human PC3 cells	[PMID: 25301770]
PC-3	EC₅₀	4300 nM Compound: 5, casodex	Displacement of [3H]R1881 from androgen receptor in human PC3 cells Displacement of [3H]R1881 from androgen receptor in human PC3 cells	[PMID: 25591066]
PC-3	GI₅₀	9.15 μM Compound: Casodex	Growth inhibition of human PC3 cells by MTT assay Growth inhibition of human PC3 cells by MTT assay	[PMID: 25634130]
PC-3	IC₅₀	60.69 μM Compound: BIC	Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay Antiproliferative activity against AR negative human PC3 cells after 48 hrs by MTT assay	[PMID: 28162857]
PC-3	IC₅₀	1.3 μM Compound: Bicalutamide	Antiproliferative activity against human PC-3 cells Antiproliferative activity against human PC-3 cells	[PMID: 33421712]
PC-3	IC₅₀	1.3 μM Compound: Bicalutamide	Antiproliferative activity against human PC-3 cells Antiproliferative activity against human PC-3 cells	[PMID: 34655985]
SAOS-2	IC₅₀	232 nM Compound: Bicalutamide	Activity at androgen receptor in human Saos2 cells assessed as IL6 repression Activity at androgen receptor in human Saos2 cells assessed as IL6 repression	[PMID: 18442912]
SC-3	IC₅₀	0.67 μM Compound: 1	Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay Antiandrogen activity against androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell proliferation by WST1 assay	[PMID: 20888766]
SC-3	IC₅₀	3 μM Compound: Bicalutamide	Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days Antagonist activity at androgen receptor in androgen-dependent mouse SC3 cells assessed as inhibition of testosterone-induced cell growth after 3 days	[PMID: 23462715]
VCaP	IC₅₀	64.712 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human VCaP cells assessed as relative inhibition after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
VCaP	IC₅₀	68.37 μM Compound: 3; Casodex; Bicalutamide	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining based fluorescence 2D monolayer assay	[PMID: 27131065]
VCaP	IC₅₀	68.37 μM Compound: RS-Bicalutamide	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by propidium iodide staining based fluorescence assay	[PMID: 27301368]
VCaP	IC₅₀	68.4 μM Compound: 1	Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay Antiproliferative activity against human VCaP cells assessed as reduction in cell growth incubated for 96 hrs by propidium iodide based 2D monolayer assay	[PMID: 31288149]
VCaP	IC₅₀	51.61 μM Compound: Bicalutamide	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability Antiproliferative activity against human VCaP cells assessed as reduction in cell viability	[PMID: 33513386]

In Vitro

Bicalutamide competes with androgens for binding AR in in a whole-cell binding-assay (LNCaP/AR(cs) cells), with an IC₅₀ of 160 nM^[1].
Bicalutamide induces proliferation of VCaP cells in a dose-dependent manner, whereas partially antagonizes the effects of R1881 (synthetic androgen)^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Bicalutamide (10 mg/kg; i.g.; daily; for 28 days) exhibits anti-tumor activity in prostate cancer mice model^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Castrate male mice, bearing LNCaP/AR(cs) xenograft tumors^[1]
Dosage:

10 mg/kg
Administration:

Oral gavage, daily, for 28 days
Result:

Inhibited tumors growth.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 90357-06-5
Appearance Solid
Masse moléculaire 430.37
Formule C₁₈H₁₄F₄N₂O₄S
Color White to off-white
SMILES

FC1=CC=C(S(=O)(CC(O)(C(NC2=CC=C(C#N)C(C(F)(F)F)=C2)=O)C)=O)C=C1
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (21)

All OthersRT-PCRHistological Imaging/StainingIF

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Journal Impact Factor

Cancer Res

Malonyl-CoA Promotes Prostate Cancer Progression and Castration Resistance by Enhancing Lipogenesis and Ran Activation. [Abstract]

2025 Aug 27. PMID: 40865048
Redox Biol

DNMT1-DUOXA1 axis discovers a novel methylation-ferroptosis circuit in bicalutamide-resistant prostate cancer. [Abstract]

2026 Jul:94:104188. PMID: 42097033
Nucleic Acids Res

The androgen receptor couples promoter recruitment of RNA processing factors to regulation of alternative polyadenylation at the 3' end of transcripts. [Abstract]

2022 Sep 23;50(17):9780-9796. PMID: 36043441

Bicalutamide purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2022 Sep 23;50(17):9780-9796. [Abstract]

KLK3 expression was evaluated in cells treated with Bicalutamide at 10μM or Enzalutamide at 1μM.

Bicalutamide purchased from MedChemExpress. Usage Cited in: Nucleic Acids Res. 2022 Sep 23;50(17):9780-9796. [Abstract]

qRT-PCR analysis of APA events in cells treated with Bicalutamide at 10μM or Enzalutamide at 1μM.
Adv Sci (Weinh)

GNL3 Orchestrates AR Transcriptional Programs to Drive Castration-Resistant Prostate Cancer and Immune Evasion. [Abstract]

2026 Mar 2:e16411. PMID: 41772945
Cell Rep Med

CAN-Scan: A multi-omic phenotype-driven precision oncology platform identifies prognostic biomarkers of therapy response for colorectal cancer. [Abstract]

2025 Apr 15;6(4):102053. PMID: 40187357
Biomaterials

Automated discovery of nanomaterials via drug aggregation induced emission. [Abstract]

2022 Oct:289:121800. PMID: 36166893
Cell Death Dis

CRISPR screening identifies CDK12 as a conservative vulnerability of prostate cancer. [Abstract]

2021 Jul 27;12(8):740. PMID: 34315855
Arterioscler Thromb Vasc Biol

FSH Is Responsible for Androgen Deprivation Therapy-Associated Atherosclerosis in Mice by Exaggerating Endothelial Inflammation and Monocyte Adhesion. [Abstract]

2024 Mar;44(3):698-719. PMID: 38205641

Bicalutamide purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]

Oil red O staining of aortic roots of mice in the saline, Leu, Deg, and Leu+Bica (Bicalutamide: 10 mg/kg) groups.

Bicalutamide purchased from MedChemExpress. Usage Cited in: Arterioscler Thromb Vasc Biol. 2024 Mar;44(3):698-719. [Abstract]

Bica (Bicalutamide: 10 mg/kg). Immunostaining of mouse aortic root plaques with SmαA (smooth muscle α-actin) (red).
RSC Adv

Three-in-one: exploration of co-encapsulation of cabazitaxel, bicalutamide and chlorin e6 in new mixed cyclodextrin-crosslinked polymers. [Abstract]

2023 Apr 6;13(16):10923-10939. PMID: 37033421
RSC Adv

Nobiletin, a citrus polymethoxyflavone, enhances the effects of bicalutamide on prostate cancer cells via down regulation of NF-κB, STAT3, and ERK activation. [Abstract]

2020 Mar 10;10(17):10254-10262. PMID: 35498570
J Drug Deliv Sci Technol

2021, 102340.
Molecules

Carboxylated Mesoporous Carbon Nanoparticles as Bicalutamide Carriers with Improved Biopharmaceutical and Chemo-Photothermal Characteristics. [Abstract]

2025 Jul 22;30(15):3055. PMID: 40807230
Sci Rep

Inhibition of androgen receptor promotes CXC-chemokine receptor 7-mediated prostate cancer cell survival. [Abstract]

2017 Jun 8;7(1):3058. PMID: 28596572

Bicalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2017 Jun 8;7(1):3058. [Abstract]

CXCR7 mRNA in cells treated with 2 µM Bicalutamide (BiC) relative to untreated (UT) cells.
PLoS Genet

Generation of prostate cancer assembloids modeling the patient-specific tumor microenvironment. [Abstract]

2025 Mar 31;21(3):e1011652. PMID: 40163511
Prostate

MIF Facilitates Resistance to Androgen Deprivation Therapy by Regulating AMPD2 Expression in Prostate Cancer Cells. [Abstract]

2025 Sep 19. PMID: 40968720
EJNMMI Res

Preclinical evaluation of PSMA expression in response to androgen receptor blockade for theranostics in prostate cancer. [Abstract]

2018 Oct 29;8(1):96. PMID: 30374743
SSRN

2025 Aug 9.
Orebro University

2024.
Aging (Albany NY)

AAT resistance-related AC007405.2 and AL354989.1 as novel diagnostic and prognostic markers in prostate cancer. [Abstract]

2024 Apr 19;16(8):7249-7266. PMID: 38643469
Res Sq

Sex differences in viral entry protein expression, host responses to SARS-CoV-2, and in vitro responses to sex steroid hormone treatment in COVID-19. [Abstract]

2020 Dec 31:rs.3.rs-100914. PMID: 33173861
RNA & Disease

2020 Apr.

Solvant et solubilité

In Vitro:

DMSO : ≥ 50 mg/mL (116.18 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.3236 mL

11.6179 mL

23.2358 mL

5 mM

0.4647 mL

2.3236 mL

4.6472 mL

10 mM

0.2324 mL

1.1618 mL

2.3236 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.81 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (274 KB)
SDS (393 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Nicola J. Clegg,1 John Wongvipat,1,2 Jim Joseph, ARN-509: a novel anti-androgen for prostate cancer treatment. Cancer Res. 2012 March 15; 72(6): 1494-1503.

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.3236 mL	11.6179 mL	23.2358 mL	58.0896 mL
	5 mM	0.4647 mL	2.3236 mL	4.6472 mL	11.6179 mL
	10 mM	0.2324 mL	1.1618 mL	2.3236 mL	5.8090 mL
	15 mM	0.1549 mL	0.7745 mL	1.5491 mL	3.8726 mL
	20 mM	0.1162 mL	0.5809 mL	1.1618 mL	2.9045 mL
	25 mM	0.0929 mL	0.4647 mL	0.9294 mL	2.3236 mL
	30 mM	0.0775 mL	0.3873 mL	0.7745 mL	1.9363 mL
	40 mM	0.0581 mL	0.2904 mL	0.5809 mL	1.4522 mL
	50 mM	0.0465 mL	0.2324 mL	0.4647 mL	1.1618 mL
	60 mM	0.0387 mL	0.1936 mL	0.3873 mL	0.9682 mL
	80 mM	0.0290 mL	0.1452 mL	0.2904 mL	0.7261 mL
	100 mM	0.0232 mL	0.1162 mL	0.2324 mL	0.5809 mL

Keywords

Bicalutamide

21 Cited Publications

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Bicalutamide

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Publications Citing Use of MedChemExpress (MCE) Bicalutamide

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bicalutamide

Bioactive Compound Library Max

Bioactive Compound Library

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

Anti-COVID-19 Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Anti-Pancreatic Cancer Compound Library

Transcription Factor-Targeted Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Off-patent Drug Library

Mitochondrial Toxicity Compound Library

Cell Death Library

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

RNA Binding Bioactive Compound Library

Publications Citing Use of MedChemExpress (MCE) Bicalutamide

Activité biologique

Chemical Information

Publications (21)

Solvant et solubilité

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Bicalutamide Related Classifications

HY-14249 Related Classifications