Bicalutamide

Name: Bicalutamide
Brand: MedChemExpress
SKU: HY-14249
Rating: 5.0 (20 reviews)

Cat. No.: HY-14249 Purity: 99.92%: Data Sheet
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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.

For research use only. We do not sell to patients.

CAS No. : 90357-06-5

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10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
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Based on 20 publication(s) in Google Scholar

Other Forms of Bicalutamide:

20 Publications Citing Use of MCE Bicalutamide

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RT-PCR

Histological Imaging/Staining

: 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).

: 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.

: 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.

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Biological Activity
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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
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	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	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-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	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	> 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 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	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	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	0.33 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	0.33 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 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	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	0.47 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]
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	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]
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	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	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]
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	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	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	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	> 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]
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	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	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	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]
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]
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]
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	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]
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	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]
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: 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	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	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]
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	0.054 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 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	0.12 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	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	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	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	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	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	1.5 μM Compound: Bicalutamide	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 33421712]
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	1000 nM 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	160 nM Compound: 55	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 35786895]
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	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	30 μM Compound: 2	Growth inhibition of human LNCAP cells Growth inhibition of human LNCAP cells	[PMID: 25301770]
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	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	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	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	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	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	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	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	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	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	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	> 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]
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	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	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]
PC-3	IC₅₀	58 μM Compound: 2	Growth inhibition of human PC3 cells Growth inhibition of human PC3 cells	[PMID: 25301770]
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	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	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	> 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]
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	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]
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]

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.

Clinical Trial

Molecular Weight

430.37

Formula

C₁₈H₁₄F₄N₂O₄S

CAS No.

90357-06-5

Appearance

Solid

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

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

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo:

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

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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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

mg/kg

Animal weight
(per animal)

Dosing volume
(per animal)

μL

Number of animals

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

Please enter your animal formula composition:

DMSO +

Tween-80 +

Saline

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.

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).

Calculation results:

Working solution concentration: mg/mL

Method for preparing stock solution: mg drug dissolved in μL DMSO (Stock solution concentration: mg/mL).

The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).

Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.

If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.

Purity & Documentation

Purity: 99.92%

Select Batch:

Data Sheet (274 KB) SDS (393 KB)

COA (250 KB) HNMR (133 KB) RP-HPLC (224 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[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.

Complete Stock Solution Preparation Table

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

Bicalutamide Related Classifications

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Bicalutamide90357-06-5Androgen ReceptorAutophagynon-steroidalandrogenreceptorprostate cancercastration-resistantprostatecanceranti-androgenInhibitorinhibitorinhibit

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