Cat. No.: HY-70002

Enzalutamide

(Synonyms: MDV3100)

220 Cited Publications

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Based on 220 publication(s) in Google Scholar

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator.

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

Purity: 99.97%
CAS No.: 915087-33-1
Formula: C₂₁H₁₆F₄N₄O₂S
Molecular Weight:464.44

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

Enzalutamide Chemical Structure

CAS No.: 915087-33-1

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Fluorescent Dye

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Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
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- In Vivo
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Chemical Information
Publications (220)
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Biological Activity

Description

Enzalutamide (MDV3100) is an androgen receptor (AR) antagonist with an IC₅₀ of 36 nM in LNCaP prostate cells. Enzalutamide is an autophagy activator^[1]^[2].

IC₅₀ & Target

IC50: 36 nM (androgen-receptor, in LNCaP cells)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
CWR22R	IC₅₀	9.7 μM Compound: 3, MDV3100	Inhibition of cell survival in human CWR22Rv1 cells after 144 hrs by TUNEL assay Inhibition of cell survival in human CWR22Rv1 cells after 144 hrs by TUNEL assay	[PMID: 25121586]
CWR22R	GI₅₀	3.34 μM Compound: MDV3100	Growth inhibition of human CWR22Rv1 cells by MTT assay Growth inhibition of human CWR22Rv1 cells by MTT assay	[PMID: 25634130]
CWR22R	IC₅₀	31.76 μM Compound: Enzalutamide	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	31.76 μM Compound: 5; MDV3100; Xtandi; Enzalutamide	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	31.76 μM Compound: 4	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	36.66 μM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human 22Rv1 cells after 72 hrs by Cell-Titer Glo assay	[PMID: 29448139]
CWR22R	IC₅₀	36.66 μM Compound: Enz	Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
CWR22R	IC₅₀	36.66 μM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human 22Rv1 cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
CWR22R	IC₅₀	24.77 μM Compound: 2a	Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human 22Rv1 cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
CWR22R	IC₅₀	>10 μM Compound: 4	Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay Cytotoxicity against AR-positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 7 days in regular culture medium by WST-8 assay	[PMID: 30629437]
CWR22R	IC₅₀	>30 μM Compound: Enza	Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay	[PMID: 30925341]
CWR22R	IC₅₀	36.66 μM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay Antiproliferative activity against human 22Rv1 cells measured after 96 hrs by celltiter-glo assay	[PMID: 30964293]
CWR22R	GI₅₀	>40 μM Compound: Enzalutamide	Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human 22Rv1 cells harboring ARE14 construct assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
CWR22R	IC₅₀	31.8 μM Compound: 2; MDV3100	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	>30 μM Compound: Enza	Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human 22Rv1 expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
CWR22R	IC₅₀	31.76 μM Compound: Enzalutamide	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	42.3 μM Compound: ENZ	Antiproliferative activity against AR-positive human 22RV1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against AR-positive human 22RV1 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33756125]
CWR22R	IC₅₀	36.66 μM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay Antiproliferative activity against human 22Rv1 cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay	[PMID: 34121397]
CWR22R	IC₅₀	38 μM Compound: Enz	Cytotoxicity against human 22Rv1 cells Cytotoxicity against human 22Rv1 cells	[PMID: 34225450]
CWR22R	IC₅₀	46.27 μM Compound: ENZa	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 72 hrs by MTT assay	[PMID: 36031018]
CWR22R	IC₅₀	36 μM Compound: ENZ	Antiproliferative activity against AR-v7 positive human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against AR-v7 positive human 22Rv1 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 36495632]
CWR22R	IC₅₀	>1000 nM Compound: Enzalutamide	Cytotoxicity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 by WST-1 assay Cytotoxicity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 by WST-1 assay	[PMID: 36960664]
CWR22R	GI₅₀	39.83 μM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human 22Rv1 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 38033250]
CWR22R	IC₅₀	45.66 μM Compound: ENZ	Cytotoxicity against human androgen-independent/androgen-responsive 22Rv1 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human androgen-independent/androgen-responsive 22Rv1 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
CWR22R	IC₅₀	36 μM Compound: ENZ	Inhibition of cell viability in ARV7-positive human 22Rv1 cells by Steady-Glo luciferase assay Inhibition of cell viability in ARV7-positive human 22Rv1 cells by Steady-Glo luciferase assay	[PMID: 38359754]
CWR22R	IC₅₀	>1000 nM Compound: Enzalutamide	Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human 22Rv1 cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
CWR22R	IC₅₀	15.6 μM Compound: Enzalutamide	Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against AR/AR-V7 positive human 22Rv1 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
CWR22R	IC₅₀	>1000 nM Compound: Enzalutamide	Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human 22Rv1 cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
DU-145	IC₅₀	32.27 μM Compound: 5; MDV3100; Xtandi; Enzalutamide	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	32.27 μM Compound: 4	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	46.1 μM Compound: Enzalutamide	Antiproliferative activity against AR negative human DU145 cells after 3 days by MTT assay Antiproliferative activity against AR negative human DU145 cells after 3 days by MTT assay	[PMID: 27810589]
DU-145	IC₅₀	46.1 μM Compound: Enzalutamide	Antiproliferative activity against human DU145 cells after 3 days by MTT assay Antiproliferative activity against human DU145 cells after 3 days by MTT assay	[PMID: 29117897]
DU-145	IC₅₀	44.55 μM Compound: 2a	Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human DU145 cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
DU-145	IC₅₀	44.7 μM Compound: Enzalutamide	Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human DU145 cells measured after 72 hrs by celltiter-glo assay	[PMID: 30964293]
DU-145	IC₅₀	32.3 μM Compound: 2; MDV3100	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	49.3 μM Compound: MDV3100	Antiproliferative activity against human DU-145 cells assessed as reduction in cel viability after 72 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as reduction in cel viability after 72 hrs by MTT assay	[PMID: 32169785]
DU-145	IC₅₀	32.27 μM Compound: Enzalutamide	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	45.3 μM Compound: ENZ	Antiproliferative activity against AR-negative human DU145 cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against AR-negative human DU145 cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33756125]
DU-145	GI₅₀	>10 μM Compound: enzalutamide	Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human DU-145 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
DU-145	GI₅₀	>31 μM Compound: Enzalutamide	Growth inhibition of human DU-145 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human DU-145 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
DU-145	IC₅₀	>50 μM Compound: 5; Enz	Cytotoxicity against androgen receptor independent human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against androgen receptor independent human DU-145 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37209451]
DU-145	GI₅₀	54.78 μM Compound: Enzalutamide	Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human DU-145 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 38033250]
DU-145	IC₅₀	121.01 μM Compound: ENZ	Cytotoxicity against human DU-145 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human DU-145 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
DU-145	IC₅₀	44.6 μM Compound: Enzalutamide	Antiproliferative activity against AR-negative human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay Antiproliferative activity against AR-negative human DU-145 cells assessed as inhibition of cell growth incubated for 48 hrs by CCK-8 assay	[PMID: 38512060]
GES1	IC₅₀	96.89 μM Compound: Enz	Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation by MTT assay Cytotoxicity against human GES1 cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36154033]
HEK293	IC₅₀	0.216 μM Compound: 5	Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay Antagonist activity at human androgen receptor expressed in HEK293 cells assessed as inhibition of R1881-induced receptor transactivation after 24 hrs by luciferase reporter gene assay	[PMID: 30525603]
L02	IC₅₀	17.1 μM Compound: Enza	Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay Antiproliferative activity against human L02 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay	[PMID: 30925341]
L02	IC₅₀	17.1 μM Compound: Enza	Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human L02 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
LNCaP	IC₅₀	>100 μM Compound: Enzalutamide	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	915 nM Compound: 6, MDV3100	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	GI₅₀	5.12 μM Compound: 6, MDV3100	Cytotoxicity against human LNCAP cells after 7 days by MTT assay Cytotoxicity against human LNCAP cells after 7 days by MTT assay	[PMID: 23713567]
LNCaP	GI₅₀	2.88 μM Compound: MDV3100	Growth inhibition of human LNCAP cells by MTT assay Growth inhibition of human LNCAP cells by MTT assay	[PMID: 25634130]
LNCaP	IC₅₀	127.1 nM Compound: 4	Antiproliferative activity against human LNCAP cells after 3 days Antiproliferative activity against human LNCAP cells after 3 days	[PMID: 26046313]
LNCaP	IC₅₀	11.47 μM Compound: 5; MDV3100; Xtandi; Enzalutamide	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	11.47 μM Compound: 4	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	EC₅₀	180 nM Compound: 4	Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control Inhibition of DHT-induced androgen receptor transactivation in human LNCaP cells after 24 hrs by luciferase reporter gene assay relative to control	[PMID: 27437082]
LNCaP	IC₅₀	4.85 μM Compound: 4	Antiproliferative activity against human LNCAP cells after 7 days by MTT assay Antiproliferative activity against human LNCAP cells after 7 days by MTT assay	[PMID: 27437082]
LNCaP	IC₅₀	12.5 μM Compound: Enzalutamide	Antiproliferative activity against human LNCAP cells after 3 days by MTT assay Antiproliferative activity against human LNCAP cells after 3 days by MTT assay	[PMID: 29117897]
LNCaP	IC₅₀	33.84 μM Compound: Enzalutamide	Antiproliferative activity against human LNCAP cells after 72 hrs by Cell-Titer Glo assay Antiproliferative activity against human LNCAP cells after 72 hrs by Cell-Titer Glo assay	[PMID: 29448139]
LNCaP	IC₅₀	33.84 μM Compound: Enz	Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
LNCaP	IC₅₀	42.37 μM Compound: Enzalutamide	Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human LNCAP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP	IC₅₀	20.9 μM Compound: 2a	Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human LNCAP cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
LNCaP	IC₅₀	25 nM Compound: 4	Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay	[PMID: 30629437]
LNCaP	IC₅₀	7.9 μM Compound: ENZa	Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell growth incubated for 72 hrs by MTT assay	[PMID: 30711833]
LNCaP	IC₅₀	1.31 μM Compound: Enzal	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by MTT assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 30743097]
LNCaP	IC₅₀	5336 nM Compound: Enza	Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay Competitive displacement of [3H]R1881 from human AR-LBD expressed in LNCaP cells incubated for 24 hrs by scintillation counting method based radioligand competitive binding assay	[PMID: 30925341]
LNCaP	IC₅₀	42.37 μM Compound: Enzalutamide	Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay Antiproliferative activity against human LNCAP cells measured after 96 hrs by celltiter-glo assay	[PMID: 30964293]
LNCaP	IC₅₀	11.5 μM Compound: 2; MDV3100	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	0.19 μM Compound: Enza	Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Antiproliferative activity against human LNCAP expressing AR assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
LNCaP	IC₅₀	150.8 nM Compound: Enzalutamide	Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay Antiproliferative activity against AR-positive human LNCAP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay	[PMID: 31804827]
LNCaP	IC₅₀	16.5 μM Compound: MDV3100	Antiproliferative activity against human LNCaP cells assessed as reduction in cel viability after 72 hrs by MTT assay Antiproliferative activity against human LNCaP cells assessed as reduction in cel viability after 72 hrs by MTT assay	[PMID: 32169785]
LNCaP	IC₅₀	1.9 μM Compound: Enzalutamide	Antiproliferative activity against hormone sensitive human LNCaP cells assessed as reduction in cell proliferation measured after 6 days by CellTiter-Glo assay Antiproliferative activity against hormone sensitive human LNCaP cells assessed as reduction in cell proliferation measured after 6 days by CellTiter-Glo assay	[PMID: 33388655]
LNCaP	IC₅₀	11.47 μM Compound: Enzalutamide	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	17.6 μM Compound: ENZ	Antiproliferative activity against AR-positive human LNCaP cells assessed as reduction in cell viability incubated for 3 days by MTT assay Antiproliferative activity against AR-positive human LNCaP cells assessed as reduction in cell viability incubated for 3 days by MTT assay	[PMID: 33756125]
LNCaP	IC₅₀	42.37 μM Compound: Enzalutamide	Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay Antiproliferative activity against human LNCaP cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay	[PMID: 34121397]
LNCaP	IC₅₀	133 nM Compound: 2	Growth inhibition of human LNCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay Growth inhibition of human LNCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay	[PMID: 34431670]
LNCaP	IC₅₀	133 nM Compound: Enzalutamide	Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay Growth inhibition of human LNCaP cells carrying AR T878A mutant assessed as cell viability by WST-8 assay	[PMID: 34473519]
LNCaP	IC₅₀	0.1 μM Compound: ENZ	Inhibition of prostate specific antigen expression in human LNCaP cells expressing ARR2PB-eGFP by immunoassay Inhibition of prostate specific antigen expression in human LNCaP cells expressing ARR2PB-eGFP by immunoassay	[PMID: 35077161]
LNCaP	IC₅₀	36 nM Compound: 68	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 35786895]
LNCaP	IC₅₀	437 nM Compound: 1	Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCAP cells assessed as reduction in cell viability measured after 6 days by CellTiter-Glo assay	[PMID: 36070471]
LNCaP	IC₅₀	0.48 μM Compound: Enz	Inhibition of PSA secretion in human LNCaP ARR2PB-eGFP cells measured after 3 days by immuno assay Inhibition of PSA secretion in human LNCaP ARR2PB-eGFP cells measured after 3 days by immuno assay	[PMID: 36154033]
LNCaP	IC₅₀	26.32 μM Compound: Enz	Cytotoxicity against human LNCAP cells assessed as inhibition of cell proliferation by MTT assay Cytotoxicity against human LNCAP cells assessed as inhibition of cell proliferation by MTT assay	[PMID: 36154033]
LNCaP	IC₅₀	52 nM Compound: Enzalutamide	Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 in charcoal stripped serum by WST-1 assay Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 in charcoal stripped serum by WST-1 assay	[PMID: 36960664]
LNCaP	IC₅₀	13.9 μM Compound: 5; Enz	Cytotoxicity against androgen receptor dependent human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Cytotoxicity against androgen receptor dependent human LNCaP cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 37209451]
LNCaP	IC₅₀	349.8 nM Compound: 2; ENZ	Antiproliferative activity against human LNCaP cells incubated for 6 days by CellTiter-Glo assay Antiproliferative activity against human LNCaP cells incubated for 6 days by CellTiter-Glo assay	[PMID: 37458396]
LNCaP	IC₅₀	213 nM Compound: Enzalutamide	Growth inhibition in human LNCaP cells assessed as reduction in cell viability Growth inhibition in human LNCaP cells assessed as reduction in cell viability	[PMID: 37683104]
LNCaP	IC₅₀	3.33 μM Compound: ENZ	Cytotoxicity against human AR-dependent LNCaP cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human AR-dependent LNCaP cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
LNCaP	IC₅₀	8000 nM Compound: Enzalutamide	Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human LNCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
LNCaP	IC₅₀	8000 nM Compound: Enzalutamide	Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human LNCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]
LNCaP C4-2	GI₅₀	>40 μM Compound: Enzalutamide	Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human C4-2 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
LNCaP C4-2B	IC₅₀	17.96 μM Compound: Enz	Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay	[PMID: 29566488]
LNCaP C4-2B	IC₅₀	20.77 μM Compound: Enzalutamide	Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human C4-2B cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
LNCaP C4-2B	IC₅₀	23.56 μM Compound: Enzalutamide	Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay Antiproliferative activity against human C4-2B cells measured after 96 hrs by celltiter-glo assay	[PMID: 30964293]
LNCaP C4-2B	IC₅₀	23.56 μM Compound: Enzalutamide	Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay Antiproliferative activity against human LNCaP C4-2B cells assessed as cell viability incubated for 96 hrs by Cell-Titer Glo assay	[PMID: 34121397]
LNCaP C4-2B	IC₅₀	18 μM Compound: Enz	Cytotoxicity against human C42B cells Cytotoxicity against human C42B cells	[PMID: 34225450]
LNCaP C4-2B	IC₅₀	22.17 μM Compound: 1	Antitumor activity against enzalutamide-resisitant human C4-2B cells administered for 3 months Antitumor activity against enzalutamide-resisitant human C4-2B cells administered for 3 months	[PMID: 36070471]
LNCaP C4-2B	IC₅₀	22.17 μM Compound: 2; ENZ	Cytotoxicity against human LNCaP C4-2B cells measured after 3 months Cytotoxicity against human LNCaP C4-2B cells measured after 3 months	[PMID: 37458396]
PC-3	GI₅₀	9.15 μM Compound: MDV3100	Growth inhibition of human PC3 cells by MTT assay Growth inhibition of human PC3 cells by MTT assay	[PMID: 25634130]
PC-3	IC₅₀	15.07 μM Compound: Enzal	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 96 hrs by MTT assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability after 96 hrs by MTT assay	[PMID: 30743097]
PC-3	IC₅₀	>30 μM Compound: Enza	Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay Antiproliferative activity against human PC3 cells assessed as reduction in cell viability incubated for 6 days by CCK8 assay	[PMID: 30925341]
PC-3	IC₅₀	53.38 μM Compound: Enzalutamide	Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay Antiproliferative activity against human PC3 cells measured after 72 hrs by celltiter-glo assay	[PMID: 30964293]
PC-3	GI₅₀	>40 μM Compound: Enzalutamide	Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-negative human PC3 cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
PC-3	IC₅₀	>30 μM Compound: Enza	Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay Cytotoxicity against human PC3 assessed as reduction in cell viability incubated for 6 days by CCK-8 assay	[PMID: 31437779]
PC-3	GI₅₀	>10 μM Compound: enzalutamide	Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as cell growth inhibition incubated for 48 hrs by MTT assay	[PMID: 34908406]
PC-3	IC₅₀	24.63 μM Compound: Enzalutamide	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth incubated for 72 hrs by MTT assay	[PMID: 35259487]
PC-3	IC₅₀	42 μM Compound: ENZ	Antiproliferative activity against human PC-3 cells measured after 3 days by celltiter-glo luminescence assay Antiproliferative activity against human PC-3 cells measured after 3 days by celltiter-glo luminescence assay	[PMID: 36495632]
PC-3	GI₅₀	22 μM Compound: Enzalutamide	Growth inhibition of human PC-3 cells measured after 24 to 72 hrs by SRB method Growth inhibition of human PC-3 cells measured after 24 to 72 hrs by SRB method	[PMID: 37163949]
PC-3	GI₅₀	73.08 μM Compound: Enzalutamide	Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay Antiproliferative activity against human PC-3 cells assessed as growth inhibition incubated for 72 hrs by CCK8 assay	[PMID: 38033250]
PC-3	IC₅₀	72.71 μM Compound: ENZ	Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 96 hrs by MTT assay Cytotoxicity against human PC-3 cells assessed as cell viability incubated for 96 hrs by MTT assay	[PMID: 38153295]
PC-3	IC₅₀	42 μM Compound: ENZ	Inhibition of cell viability in AR-independent human PC-3 cells by Steady-Glo luciferase assay Inhibition of cell viability in AR-independent human PC-3 cells by Steady-Glo luciferase assay	[PMID: 38359754]
RWPE-1	IC₅₀	>40 μM Compound: Enz	Cytotoxicity against human RWPE-1 cells Cytotoxicity against human RWPE-1 cells	[PMID: 34225450]
VCaP	GI₅₀	0.61 μM Compound: 3, MDV3100	Growth inhibition of human VCaP cells after 144 hrs by SRB assay Growth inhibition of human VCaP cells after 144 hrs by SRB assay	[PMID: 25121586]
VCaP	IC₅₀	53.04 μM Compound: 5; MDV3100; Xtandi; Enzalutamide	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	53.04 μM Compound: 4	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	>30 μM Compound: Enzalutamide	Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay Antiproliferative activity against human VCaP cells treated at 12 hrs post cell seeding measured at 72 to 144 hrs post cell seeding by Cell-Titer Glo assay	[PMID: 29758518]
VCaP	IC₅₀	24.47 μM Compound: 2a	Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining-based fluorescence assay Antiproliferative activity against human VCaP cells after 96 hrs by propidium iodide staining-based fluorescence assay	[PMID: 30108852]
VCaP	IC₅₀	87.4 nM Compound: 4	Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay Cytotoxicity against AR-positive human VCaP cells assessed as inhibition of cell growth incubated for 7 days in presence of AR agonist, R1881 in charcoal stripped medium by WST-8 assay	[PMID: 30629437]
VCaP	IC₅₀	3.66 μM Compound: Enzal	Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by MTS assay Antiproliferative activity against human VCaP cells assessed as reduction in cell viability after 96 hrs by MTS assay	[PMID: 30743097]
VCaP	GI₅₀	>40 μM Compound: Enzalutamide	Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay Antiproliferative activity against AR-positive human VCaP cells assessed as growth inhibition after 72 hrs by resazurin dye based fluorescence assay	[PMID: 31271960]
VCaP	IC₅₀	53 μM Compound: 2; MDV3100	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	364 nM Compound: Enzalutamide	Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay Antiproliferative activity against AR- positive human VCaP cells incubated for 7 days in presence of AR agonist, R1881 by WST-8 assay	[PMID: 31804827]
VCaP	IC₅₀	149 nM Compound: 1; MDV-3100	Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay	[PMID: 33470111]
VCaP	IC₅₀	53.04 μM Compound: Enzalutamide	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	149 nM Compound: 1; MDV-3100	Antiproliferative activity against human VCaP cells expressing wild type AR assessed as reduction in R1881-stimulated cell proliferation measured after 5 days by Celltiter-Glo luminescence assay Antiproliferative activity against human VCaP cells expressing wild type AR assessed as reduction in R1881-stimulated cell proliferation measured after 5 days by Celltiter-Glo luminescence assay	[PMID: 34422225]
VCaP	IC₅₀	394 nM Compound: 2	Growth inhibition of human VCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay Growth inhibition of human VCaP cells assessed as cell viability measured after 4 days in presence of R1881 by WST-8 assay	[PMID: 34431670]
VCaP	IC₅₀	393 nM Compound: Enzalutamide	Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay Growth inhibition of human VCaP cells assessed as cell viability by WST-8 assay	[PMID: 34473519]
VCaP	IC₅₀	>1000 nM Compound: Enzalutamide	Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay Antiproliferative activity against human VCaP cells assessed as cell growth inhibition incubated for 4 days by celtiter-glo luminescent assay	[PMID: 38477974]
VCaP	IC₅₀	9500 nM Compound: Enzalutamide	Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay Antiproliferative activity against AR positive human VCaP cells assessed inhibition of cell growth measured after 4 days by CellTiter-Glo Luminescent cell viability assay	[PMID: 38530938]

In Vitro

Enzalutamide (MDV3100) has greater affinity to AR than ICI 176334 does in a competition assay with 16β-[¹⁸F]fluoro-5α-DHT (18-FDHT) in castration-resistant LNCaP/AR cells (AR-overexpressing). While Enzalutamide shows no agonism in LNCaP/AR prostate cells. Enzalutamide antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. Enzalutamide inhibits the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys)^[1].
Enzalutamide also prevents nuclear translocation and co-activator recruitment of the ligand-receptor complex^[2].

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

In Vivo

Enzalutamide (MDV3100) induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg^[1].
Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg^[4].

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

Clinical Trial

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

Chemical Information

CAS No. 915087-33-1
Appearance Solid
Molecular Weight 464.44
Formula C₂₁H₁₆F₄N₄O₂S
Color White to off-white
SMILES

S=C(N(C(C1(C)C)=O)C2=CC=C(C#N)C(C(F)(F)F)=C2)N1C3=CC(F)=C(C(NC)=O)C=C3
Synonyms

MDV3100
Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Publications (220)

All IFWBCell Proliferation/Viability Assay

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Journal Impact Factor

Nature

Androgen activity in the male embryonic hindbrain drives lethal PFA ependymoma. [Abstract]

2026 Apr;652(8110):763-773. PMID: 41882358
Cancer Cell

Small-molecule RNA therapeutics to target prostate cancer. [Abstract]

2025 Mar 18:S1535-6108(25)00079-0. PMID: 40118049
Cell

Ferroptosis surveillance independent of GPX4 and differentially regulated by sex hormones. [Abstract]

2023 Jun 22;186(13):2748-2764.e22. PMID: 37267948

Enzalutamide purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 22;186(13):2748-2764.e22. [Abstract]

Viability analysis of LnAR cells harboring vector or MBOAT2 overexpression. Cells were pretreated with DMSO (ctrl) or 5 μM ENZ (Enzalutamide) for 48 h, followed by 1 μM RSL3 for 24 h.

Enzalutamide purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 22;186(13):2748-2764.e22. [Abstract]

Western blot showing expression of endogenous and ectopic MBOAT2 in LnAR cells harboring either vector control or MBOAT2-mCherry. Cells were treated with 5 μM ENZ (Enzalutamide) as indicated for 48 h.
Cancer Discov

Serotonin modulates lineage plasticity in neuroendocrine prostate cancer via epigenetic reprogramming. [Abstract]

2025 Dec 19. PMID: 41416996
Cancer Discov

The Master Neural Transcription Factor BRN2 Is an Androgen Receptor-Suppressed Driver of Neuroendocrine Differentiation in Prostate Cancer. [Abstract]

2017 Jan;7(1):54-71. PMID: 27784708

Enzalutamide purchased from MedChemExpress. Usage Cited in: Cancer Discov. 2017 Jan;7(1):54-71. [Abstract]

BRN2 expression inversely correlates with PSA in human PCa and is induced by ENZ. Protein and relative mRNA expression of BRN2, SYP, NSE, CGA, and VINC in siScr and 796 siBRN2 16D^CRPC cells treated -/+ 10 μM ENZ for 2, 4 or 7 days.
Cancer Res

MECOM Function is Critical for AR-Driven Treatment-Resistant Prostate Cancer. [Abstract]

2026 Jan 13. PMID: 41529070
Cancer Res

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

2025 Aug 27. PMID: 40865048
Cancer Res

Caloric Restriction Enhances the Efficacy of Anti-Androgen Therapy in Prostate Cancer by Inhibiting Androgen Receptor Translation. [Abstract]

2025 Aug 8. PMID: 40779415
Cancer Res

Loss of a Negative Feedback Loop between IRF8 and AR Promotes Prostate Cancer Growth and Enzalutamide Resistance. [Abstract]

2020 Jul 1;80(13):2927-2939. PMID: 32341037
Cancer Res

Heterochromatin Protein 1α Mediates Development and Aggressiveness of Neuroendocrine Prostate Cancer. [Abstract]

2018 May 15;78(10):2691-2704. PMID: 29487201
Cancer Res

UGT2B17 Expedites Progression of Castration-Resistant Prostate Cancers by Promoting Ligand-Independent AR Signaling. [Abstract]

2016 Nov 15;76(22):6701-6711. PMID: 27659047
Cancer Res

Cotargeting Androgen Receptor and Clusterin Delays Castrate-Resistant Prostate Cancer Progression by Inhibiting Adaptive Stress Response and AR Stability. [Abstract]

2013 Aug 15;73(16):5206-17. PMID: 23786771

Enzalutamide purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 Aug 15;73(16):5206-17. [Abstract]

CLU is induced by MDV3100 in time- and dose-dependent manner. LNCaP cells are treated with MDV3100 at indicated time (left) or concentration (right) and Western blot analysis is conducted with CLU, AR, and PSA antibodies.

Enzalutamide purchased from MedChemExpress. Usage Cited in: Cancer Res. 2013 Aug 15;73(16):5206-17. [Abstract]

MDV3100-induced CLU is mediated via p90Rsk-YB-1 signaling pathway. MDV3100 activates AKT and MAPK pathways. LNCaP cells are treated with 10 μM MDV3100 for indicated times and Western blotted using CLU, p-Rsk/R/Rsk, p-S6K/S6K, and pYB-1/YB-1. Vinculin is used as a loading control.
Nat Commun

AR+TREM2+ macrophage induced pathogenic immunosuppression promotes prostate cancer progression. [Abstract]

2025 Jul 29;16(1):6964. PMID: 40730555
Nat Commun

Epigenome-wide impact of MAT2A sustains the androgen-indifferent state and confers synthetic vulnerability in ERG fusion-positive prostate cancer. [Abstract]

2024 Aug 6;15(1):6672. PMID: 39107274
Nat Commun

Opposing transcriptional programs of KLF5 and AR emerge during therapy for advanced prostate cancer. [Abstract]

2021 Nov 4;12(1):6377. PMID: 34737261
Nat Commun

Androgen deprivation upregulates SPINK1 expression and potentiates cellular plasticity in prostate cancer. [Abstract]

2020 Jan 20;11(1):384. PMID: 31959826
Nat Commun

Single-cell ATAC and RNA sequencing reveal pre-existing and persistent cells associated with prostate cancer relapse. [Abstract]

2021 Sep 6;12(1):5307. PMID: 34489465
Nat Commun

The MAO inhibitors phenelzine and clorgyline revert enzalutamide resistance in castration resistant prostate cancer. [Abstract]

2020 Jun 1;11(1):2689. PMID: 32483206
Nat Commun

Genetic characterization of a unique neuroendocrine transdifferentiation prostate circulating tumor cell-derived eXplant model. [Abstract]

2020 Apr 20;11(1):1884. PMID: 32313004
Acta Pharm Sin B

A novel inhibitor of ARfl and ARv7 induces protein degradation to overcome enzalutamide resistance in advanced prostate cancer. [Abstract]

2022 Nov;12(11):4165-4179. PMID: 36386477
Adv Sci (Weinh)

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

2026 Mar 2:e16411. PMID: 41772945
Adv Sci (Weinh)

Cancer Cell-Intrinsic Cholesterol Induces Lipid-Associated Macrophage Differentiation via SP1 Palmitoylation to Promote Prostate Cancer Progression. [Abstract]

2026 Apr;13(19):e08588. PMID: 41603134
Adv Sci (Weinh)

Primary Cilia Formation Mediated by Hsa_Circ_0005185/OTUB1/RAB8A Complex Inhibits Prostate Cancer Progression by Suppressing Hedgehog Signaling Pathway. [Abstract]

2025 Jan 9:e2411675. PMID: 39785769
Adv Sci (Weinh)

Osteoblast-Derived ECM1 Promotes Anti-Androgen Resistance in Bone Metastatic Prostate Cancer. [Abstract]

2024 Nov 20:e2407662. PMID: 39563492
Adv Sci (Weinh)

Enzalutamide Sensitizes Castration-Resistant Prostate Cancer to Copper-Mediated Cell Death. [Abstract]

2024 Jun 10:e2401396. PMID: 38859590
Adv Sci (Weinh)

Identification of PRDX5 as A Target for The Treatment of Castration-Resistant Prostate Cancer. [Abstract]

2024 Mar;11(9):e2304939. PMID: 38115765
Nat Chem Biol

Plasma membrane-associated ARAF condensates fuel RAS-related cancer drug resistance. [Abstract]

2025 Aug;21(8):1226-1237. PMID: 39870764
J Clin Invest

Targeting Wnt/β-Catenin and circadian regulator restores PRC2/EZH2 controlled chromatin bivalency and suppresses cell state diversity. [Abstract]

2026 Mar 17:e200260. PMID: 41842971
J Clin Invest

PRMT5-mediated FUBP1 methylation accelerates prostate cancer progression. [Abstract]

2024 Aug 15:e175023. PMID: 39146021
J Clin Invest

Ivermectin inhibits HSP27 and potentiates efficacy of oncogene targeting in tumor models. [Abstract]

2020 Feb 3;130(2):699-714. PMID: 31845908
Theranostics

A transcriptional biosensor to monitor single cancer cell therapeutic responses by bioluminescence microscopy. [Abstract]

2022 Jan 1;12(2):474-492. PMID: 34976196
Theranostics

ACSS3 represses prostate cancer progression through downregulating lipid droplet-associated protein PLIN3. [Abstract]

2021 Jan 1;11(2):841-860. PMID: 33391508
J Exp Clin Cancer Res

PAX6 promotes neuroendocrine phenotypes of prostate cancer via enhancing MET/STAT5A-mediated chromatin accessibility. [Abstract]

2024 May 15;43(1):144. PMID: 38745318
J Exp Clin Cancer Res

PPFIA4 promotes castration-resistant prostate cancer by enhancing mitochondrial metabolism through MTHFD2. [Abstract]

2022 Apr 5;41(1):125. PMID: 35382861
J Exp Clin Cancer Res

The DNA/RNA helicase DHX9 contributes to the transcriptional program of the androgen receptor in prostate cancer. [Abstract]

2022 May 19;41(1):178. PMID: 35590370
Sci Adv

Acute BRCAness induction and AR pathway blockage through CDK12/7/9 degradation enhances PARP inhibitor sensitivity in prostate cancer. [Abstract]

Sci Adv. 2025 Apr 25;11(17):eadu0847. PMID: 40267193
Sci Adv

Stromal-derived MAOB promotes prostate cancer growth and progression. [Abstract]

2024 Feb 9;10(6):eadi4935. PMID: 38335292
Sci Adv

A MYC inhibitor selectively alters the MYC and MAX cistromes and modulates the epigenomic landscape to regulate target gene expression. [Abstract]

2022 Apr 29;8(17):eabh3635. PMID: 35476451
J Biomed Sci

Reciprocal deregulation of NKX3.1 and AURKA axis in castration-resistant prostate cancer and NEPC models. [Abstract]

2021 Oct 8;28(1):68. PMID: 34625072
EBioMedicine

Preclinical study using androgen receptor (AR) degradation enhancer to increase radiotherapy efficacy via targeting radiation-increased AR to better suppress prostate cancer progression. [Abstract]

2019 Feb:40:504-516. PMID: 30692044
Cell Rep Med

Epigenetic profiling identifies markers of endocrine resistance and therapeutic options for metastatic castration-resistant prostate cancer. [Abstract]

2025 Jul 15;6(7):102215. PMID: 40609538
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 2:102053. PMID: 40187357
Clin Cancer Res

Targeting Prostate Cancer Subtype 1 by Forkhead Box M1 Pathway Inhibition. [Abstract]

2017 Nov 15;23(22):6923-6933. PMID: 28899970
Clin Cancer Res

siRNA Lipid Nanoparticle Potently Silences Clusterin and Delays Progression When Combined with Androgen Receptor Cotargeting in Enzalutamide-Resistant Prostate Cancer. [Abstract]

2015 Nov 1;21(21):4845-55. PMID: 26106075
Clin Cancer Res

Generation 2.5 antisense oligonucleotides targeting the androgen receptor and its splice variants suppress enzalutamide-resistant prostate cancer cell growth. [Abstract]

2015 Apr 1;21(7):1675-87. PMID: 25634993
Clin Cancer Res

Applications of immunoPET: using 124I-anti-PSCA A11 minibody for imaging disease progression and response to therapy in mouse xenograft models of prostate cancer. [Abstract]

2014 Dec 15;20(24):6367-78. PMID: 25326233
Mol Biomed

Histone methyltransferase KMT2D targets the SPOP-G3BP1 axis to enhance AR stability and drive castration-resistant prostate cancer progression. [Abstract]

2025 Nov 17;6(1):112. PMID: 41247636
Cancer Lett

Selectively targeting the dimerization interface of human androgen receptor with small-molecules to treat castration-resistant prostate cancer. [Abstract]

2018 Nov 28:437:35-43. PMID: 30165195
Int J Biol Sci

PiRNA-4447944 promotes castration-resistant growth and metastasis of prostate cancer by inhibiting NEFH expression through forming the piRNA-4447944-PIWIL2-NEFH complex. [Abstract]

2024 Jul 1;20(9):3638-3655. PMID: 38993562
Int J Biol Sci

Combined Androgen receptor blockade overcomes the resistance of breast cancer cells to palbociclib. [Abstract]

2019 Jan 1;15(3):522-532. PMID: 30745839
Cell Death Dis

Targeting valine catabolism to inhibit metabolic reprogramming in prostate cancer. [Abstract]

2024 Jul 18;15(7):513. PMID: 39025852
Cell Death Dis

A potassium-chloride co-transporter promotes tumor progression and castration resistance of prostate cancer through m6A reader YTHDC1. [Abstract]

2023 Jan 6;14(1):7. PMID: 36609444
Cell Death Dis

N-glycosylation of GDF15 abolishes its inhibitory effect on EGFR in AR inhibitor-resistant prostate cancer cells. [Abstract]

2022 Jul 19;13(7):626. PMID: 35853851
Cell Death Dis

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

2021 Jul 27;12(8):740. PMID: 34315855
Cell Death Dis

The androgen receptor mediates antiapoptotic function in myometrial cells. [Abstract]

2014 Jul 17;5(7):e1338. PMID: 25032861
Sci China Life Sci

Androgen induces 3'UTR shortening of de novo lipogenesis genes by alternative polyadenylation in prostate cancer cells. [Abstract]

2025 Jul 8. PMID: 40643802
Proc Natl Acad Sci U S A

A PHF19-YTHDC1 condensate switches EZH2-mediated gene suppression to activation for prostate cancer progression. [Abstract]

2025 Oct 28;122(43):e2510386122. PMID: 41129231
Proc Natl Acad Sci U S A

Androgen receptors in corticotropin-releasing hormone neurons mediate the sexual dimorphism in restraint-induced thymic atrophy. [Abstract]

2025 Mar 25;122(12):e2426107122. PMID: 40106355
Cell Commun Signal

Reciprocal regulation between RACGAP1 and AR contributes to endocrine therapy resistance in prostate cancer. [Abstract]

2024 Jun 19;22(1):339. PMID: 38898473
Cell Commun Signal

Cancer-associated fibroblasts promote prostate tumor growth and progression through upregulation of cholesterol and steroid biosynthesis. [Abstract]

2020 Jan 24;18(1):11. PMID: 31980029
Cell Commun Signal

MIIP inhibits the growth of prostate cancer via interaction with PP1α and negative modulation of AKT signaling. [Abstract]

2019 May 15;17(1):44. PMID: 31092266
Int J Biol Macromol

Prebiotic stachyose inhibits PRDX5 activity and castration-resistant prostate cancer development. [Abstract]

2024 Aug 19:134844. PMID: 39168191
EMBO J

YAP antagonizes TEAD-mediated AR signaling and prostate cancer growth. [Abstract]

2023 Feb 15;42(4):e112184. PMID: 36588499
Apoptosis

Insulin-like growth factor binding protein-3 serves as a biomarker for resistance to enzalutamide in prostate cancer. [Abstract]

2026 Mar 22;31(4):109. PMID: 41866645
Apoptosis

Loss of AR-regulated AFF3 contributes to prostate cancer progression and reduces ferroptosis sensitivity by downregulating ACSL4 based on single-cell sequencing analysis. [Abstract]

2024 Oct;29(9-10):1679-1695. PMID: 38478171
NPJ Precis Oncol

Transcriptional profiling clarifies a program of enzalutamide extreme non-response in lethal prostate cancer. [Abstract]

2025 Jul 7;9(1):223. PMID: 40624104
NPJ Precis Oncol

Optimized culturing yields high success rates and preserves molecular heterogeneity, enabling personalized screening for high-grade gliomas. [Abstract]

2025 May 27;9(1):156. PMID: 40425813
Neoplasia

A trio of tumor suppressor miRNA downregulates CREB5 dependent transcription to modulate neoadjuvant hormonal therapy sensitivity. [Abstract]

2023 Feb:36:100875. PMID: 36603462
NPJ Breast Cancer

Transcriptomic analysis to uncover the mechanism of radiosensitization of AR-positive triple-negative breast cancers with AR inhibition. [Abstract]

2026 Feb 24. PMID: 41735341
Eur J Nucl Med Mol Imaging

Preclinical and first-in-human evaluation of novel androgen receptor-targeted PET imaging in prostate cancer. [Abstract]

2025 Sep 23. PMID: 40986091
J Transl Med

A novel lncRNA FLJ promotes castration resistance in prostate cancer through AR mediated autophagy. [Abstract]

2025 Mar 3;23(1):255. PMID: 40033417
Biomed Pharmacother

Design, synthesis and biological evaluation of dual inhibitors targeting AR/AR-Vs and PARP1 in castration resistant prostate cancer therapy. [Abstract]

2024 Nov:180:117485. PMID: 39326103
Biomed Pharmacother

Inhibition of autophagy enhances the anticancer effect of enzalutamide on bladder cancer. [Abstract]

2019 Dec;120:109490. PMID: 31574376
Oncogene

Chaperone-mediated autophagy promotes PCa survival during ARPI through selective proteome remodeling. [Abstract]

2023 Mar;42(10):748-758. PMID: 36611121
Oncogene

TRIM59 is suppressed by androgen receptor and acts to promote lineage plasticity and treatment-induced neuroendocrine differentiation in prostate cancer. [Abstract]

2023 Feb;42(8):559-571. PMID: 36544044
Oncogene

RUVBL1 promotes enzalutamide resistance of prostate tumors through the PLXNA1-CRAF-MAPK pathway. [Abstract]

2022 Jun;41(23):3239-3250. PMID: 35508542
Oncogene

Targeting a splicing-mediated drug resistance mechanism in prostate cancer by inhibiting transcriptional regulation by PKCβ1. [Abstract]

2022 Mar;41(11):1536-1549. PMID: 35087237
Oncogene

Circular RNAs add diversity to androgen receptor isoform repertoire in castration-resistant prostate cancer. [Abstract]

2019 Nov;38(45):7060-7072. PMID: 31409897
Oncogene

Non-canonical activation of hedgehog in prostate cancer cells mediated by the interaction of transcriptionally active androgen receptor proteins with Gli3. [Abstract]

2018 Apr;37(17):2313-2325. PMID: 29429990
Oncogene

Mechanisms of the androgen receptor splicing in prostate cancer cells. [Abstract]

2014 Jun 12;33(24):3140-50. PMID: 23851510
Cell Death Discov

Tautomycin and enzalutamide combination yields synergistic effects on castration-resistant prostate cancer. [Abstract]

2022 Nov 29;8(1):471. PMID: 36446767
Cell Rep

Numb/Parkin-directed mitochondrial fitness governs cancer cell fate via metabolic regulation of histone lactylation. [Abstract]

2023 Jan 30;42(2):112033. PMID: 36724072
Br J Cancer

Nuclear FGF2, androgen receptor and Wnt pathway activation define a targetable subset of antiprogestin-resistant luminal breast cancer. [Abstract]

2026 Jun;134(11):1671-1682. PMID: 41935240
Br J Cancer

Senescence-related gene signature predicts prostate cancer progression and identifies PCNA as a therapeutic target via multi-omics machine learning integration. [Abstract]

2025 Dec 18. PMID: 41407876
Br J Cancer

Elevated serum levels of GPX4, NDUFS4, PRDX5, and TXNRD2 as predictive biomarkers for castration resistance in prostate cancer patients: an exploratory study. [Abstract]

2025 Apr;132(6):543-557. PMID: 39900986
Clin Transl Med

Androgen-repressed lncRNA LINC01126 drives castration-resistant prostate cancer by regulating the switch between O-GlcNAcylation and phosphorylation of androgen receptor. [Abstract]

2024 Jan;14(1):e1531. PMID: 38214432
Br J Cancer

Androgen and oestrogen receptor co-expression determines the efficacy of hormone receptor-mediated radiosensitisation in breast cancer. [Abstract]

2022 Sep;127(5):927-936. PMID: 35618789
Clin Transl Med

Melatonin inhibits lipid accumulation to repress prostate cancer progression by mediating the epigenetic modification of CES1. [Abstract]

2021 Jun;11(6):e449. PMID: 34185414
Sci Signal

The kinase PLK1 promotes Hedgehog signaling-dependent resistance to the antiandrogen enzalutamide in metastatic prostate cancer. [Abstract]

2025 Mar 18;18(878):eadi5174. PMID: 40100956
Antioxidants (Basel)

Characterization of the Peroxisomal Proteome and Redox Balance in Human Prostate Cancer Cell Lines. [Abstract]

2024 Nov 1;13(11):1340. PMID: 39594482
Cell Mol Life Sci

ZNF711 promotes enzalutamide resistance through transcriptional and epigenetic modification of the androgen receptor signaling pathway. [Abstract]

2026 Feb 9;83(1):103. PMID: 41656388
Cell Mol Life Sci

EP300/CREBBP acetyltransferase inhibition limits steroid receptor and FOXA1 signaling in prostate cancer cells. [Abstract]

2024 Apr 2;81(1):160. PMID: 38564048
Antioxid Redox Signal

Androgen Receptor Mediates Dopamine Agonist Resistance by Regulating Intracellular Reactive Oxygen Species in Prolactin-Secreting Pituitary Adenoma. [Abstract]

2025 Jun;42(16-18):954-972. PMID: 39360800
JCI Insight

Targeting castration-resistant prostate cancer with androgen receptor antisense oligonucleotide therapy. [Abstract]

2019 Sep 5;4(17):e122688. PMID: 31484823
Cancer Cell Int

Abiraterone and MDV3100 inhibits the proliferation and promotes the apoptosis of prostate cancer cells through mitophagy. [Abstract]

2019 Dec 10;19:332. PMID: 31827406
Eur J Med Chem

Small molecule-induced degradation of the full length and V7 truncated variant forms of human androgen receptor. [Abstract]

2018 Sep 5:157:1164-1173. PMID: 30193215

Enzalutamide purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Sep 5:157:1164-1173. [Abstract]

Dose-response curves of active degraders and Enzalutamide on AR transcriptional activity as measured in LNCaP-eGFP cells following 0.1 nM R1881 for 72 hours in RPMI+CSS media (3 replicates per point). (B) PSA inhibition curves against transcriptional activity of AR as measured from the media of LNCaP-eGFP cells with active degraders and enzalutamide under the same conditions as A.
Chin Med

Atractylenolide I ameliorated the growth and enzalutamide resistance of castration-resistant prostate cancer by targeting KIF15. [Abstract]

2025 Mar 14;20(1):35. PMID: 40087774
Biosensors (Basel)

An Extracellular Matrix Overlay Model for Bioluminescence Microscopy to Measure Single-Cell Heterogeneous Responses to Antiandrogens in Prostate Cancer Cells. [Abstract]

2024 Apr 5;14(4):175. PMID: 38667168
Mol Cancer Ther

Enzalutamide-Induced Feed-Forward Signaling Loop Promotes Therapy-Resistant Prostate Cancer Growth Providing an Exploitable Molecular Target for Jak2 Inhibitors. [Abstract]

2020 Jan;19(1):231-246. PMID: 31548294
Mol Cancer Ther

Bypassing Drug Resistance Mechanisms of Prostate Cancer with Small Molecules that Target Androgen Receptor-Chromatin Interactions. [Abstract]

2017 Oct;16(10):2281-2291. PMID: 28775145

Enzalutamide purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2281-2291. [Abstract]

Top-Cells (RPMI+CSS) are co-transfected with ARR3tk-Luc and Renilla-Luc plasmids (48 hrs). With the exception of 22Rv1, 0.1 nM R1881 is used to stimulate the AR, followed by compound treatment (24 hrs). 100% refers to normalized luminescence without compound (DMSO vehicle). Curves are fitted to a sigmoid dose-response with variable slope equation (GraphPad).
Mol Cancer Ther

Cotargeting HSP90 and Its Client Proteins for Treatment of Prostate Cancer. [Abstract]

2016 Sep;15(9):2107-18. PMID: 27390342

Enzalutamide purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18. [Abstract]

Combination of Enzalutamide and 17-AAG lead to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.
Mol Cancer Ther

Inhibition of Stat5a/b Enhances Proteasomal Degradation of Androgen Receptor Liganded by Antiandrogens in Prostate Cancer. [Abstract]

2015 Mar;14(3):713-26. PMID: 25552366
Mol Cancer Ther

A novel antiandrogen, Compound 30, suppresses castration-resistant and MDV3100-resistant prostate cancer growth in vitro and in vivo. [Abstract]

2013 May;12(5):567-76. PMID: 23493310

Enzalutamide purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2013 May;12(5):567-76. [Abstract]

LNCaP cells are treated with Compound 30 or MDV3100 for 24 hours; AR and PSA are analyzed by Western blot analysis; Vinculin is used as a loading control.

Enzalutamide purchased from MedChemExpress. Usage Cited in: Mol Cancer Ther. 2013 May;12(5):567-76. [Abstract]

LNCaP cells are maintained in androgen-deprived conditions for 24 hours and treated with 10 μM Compound 30 or MDV3100 for 2 hours followed by addition of 1 nM of R1881. After 15 minutes incubation, cells are fixed and AR localization is assessed by immunofluorescence imaging.
Nanoscale

The memristive effect as a novelty in drug monitoring. [Abstract]

2017 Jul 13;9(27):9676-9684. PMID: 28675222
Cancer Gene Ther

Targeting the androgen receptor to enhance NK cell killing efficacy in bladder cancer by modulating ADAR2/circ_0001005/PD-L1 signaling. [Abstract]

2022 Dec;29(12):1988-2000. PMID: 35915245
Int J Oncol

Enzalutamide inhibits proliferation of gemcitabine-resistant bladder cancer cells with increased androgen receptor expression. [Abstract]

2017 Jan;50(1):75-84. PMID: 27909718

Enzalutamide purchased from MedChemExpress. Usage Cited in: Int J Oncol. 2017 Jan;50(1):75-84. [Abstract]

Effects of culture in CSS and treatment with Enzalutamide on cell cycle of T24GR cells. T24 and T24GR cells (5x10⁵) are seeded in a 6-well plate and cultured for 24 h. The culture medium is changed to that containing 50 μM Enzalutamide or vehicle (DMSO). Seventy-two hours later, cell lysates are harvested and subjected to western blot analysis for cyclin B1, D1 and β-actin.
Int J Mol Sci

Cancer-Associated Fibroblasts Modify the Response of Prostate Cancer Cells to Androgen and Anti-Androgens in Three-Dimensional Spheroid Culture. [Abstract]

2016 Sep 1;17(9). pii: E1458. PMID: 27598125
Int J Cancer

Proteome profiling of enzalutamide-resistant cell lines and serum analysis identified ALCAM as marker of resistance in castration-resistant prostate cancer. [Abstract]

2022 Oct 15;151(8):1405-1419. PMID: 35689436
Mol Cancer Res

IL8 Expression Is Associated with Prostate Cancer Aggressiveness and Androgen Receptor Loss in Primary and Metastatic Prostate Cancer. [Abstract]

2020 Jan;18(1):153-165. PMID: 31604846
Int J Cancer

Pharmacological inhibition of the Notch pathway enhances the efficacy of androgen deprivation therapy for prostate cancer. [Abstract]

2018 Aug 1;143(3):645-656. PMID: 29488214

Enzalutamide purchased from MedChemExpress. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656. [Abstract]

Evaluation of protein expression change of Notch receptors response to the treatment of 10 μM Enzalutamide as an androgen receptor (AR) antagonist.
Mol Cancer Res

SOCS3 Modulates the Response to Enzalutamide and Is Regulated by Androgen Receptor Signaling and CpG Methylation in Prostate Cancer Cells. [Abstract]

2016 Jun;14(6):574-85. PMID: 27053681

Enzalutamide purchased from MedChemExpress. Usage Cited in: Mol Cancer Res. 2016 Jun;14(6):574-85. [Abstract]

LNCaP and DuCaP cells are 1 treated for 72 hours with 1 or 10 μM Enzalutamide in the presence of increasing IL6 concentrations. The effect on JAK/STAT3 signaling is measured by determining STAT3 Tyr705-phosphorylation via Western blot and calculation of dose response curves.
Toxicology

In silico, In vitro and in vivo studies: Dibutyl phthalate promotes prostate cancer cell proliferation by activating Forkhead Box M1 and remission after Natura-α pretreatment. [Abstract]

2023 Apr:488:153465. PMID: 36828243
Mol Pharm

Targeted Delivery of AR-V7 siRNA with Bivalent PSMA Aptamers Effectively Suppresses the Growth of Enzalutamide-Resistant Prostate Cancer. [Abstract]

2024 Nov 4;21(11):5749-5760. PMID: 39388218
Eur Urol Open Sci

Combining Antiandrogens with Immunotherapy for Bladder Cancer Treatment. [Abstract]

2022 Jul 26:43:35-44. PMID: 36246841
Cancers (Basel)

Inhibition of Serum Response Factor Improves Response to Enzalutamide in Prostate Cancer. [Abstract]

2020 Nov 27;12(12):3540. PMID: 33260953
Cancers

Dual Inhibitory Action of a Novel AKR1C3 Inhibitor on Both Full-Length AR and the Variant AR-V7 in Enzalutamide Resistant Metastatic Castration Resistant Prostate Cancer. [Abstract]

2020 Jul 28;12(8):2092. PMID: 32731472
Cancers

KLF5 Is Crucial for Androgen-AR Signaling to Transactivate Genes and Promote Cell Proliferation in Prostate Cancer Cells. [Abstract]

2020 Mar 21;12(3):748. PMID: 32245249
Cancers (Basel)

The Impact of Cand1 in Prostate Cancer. [Abstract]

2020 Feb 12;12(2):428. PMID: 32059441
Cancer Sci

SYT4 binds to SNAP25 to facilitate exosomal secretion and prostate cancer enzalutamide resistance. [Abstract]

2024 Aug;115(8):2630-2645. PMID: 38889208
J Cell Mol Med

GOLM1 promotes prostate cancer progression via interaction with PSMD1 and enhancing AR-driven transcriptional activation. [Abstract]

2024 Oct;28(20):e70186. PMID: 39470578
Lab Invest

Androgen receptor transcriptionally inhibits programmed death ligand-1 (PD-L1) expression and influences immune escape in bladder cancer. [Abstract]

2023 Jul;103(7):100148. PMID: 37059268
Comput Struct Biotechnol J

Identification of a Novel Trifluoromethyl-Bearing Flavonoid as a Promising Androgen Receptor Antagonist: Structure-Based Virtual Screening and In Vitro Study. [Abstract]

2026 Apr 13;35(1):0038. PMID: 41993879
Transl Oncol

The STAT3 inhibitor GPB730 enhances the sensitivity to enzalutamide in prostate cancer cells. [Abstract]

2022 Oct:24:101495. PMID: 35917644
Drug Metab Dispos

2025 Dec 22.
Drug Metab Dispos

Quantitative clinical risk assessment of CYP2C, UDP-glucuronosyltransferase, P-glycoprotein induction, and complex drug-drug interactions using TruVivo human hepatocyte triculture platform. [Abstract]

2025 Apr;53(4):100052. PMID: 40133023
Target Oncol

FT-6876, a Potent and Selective Inhibitor of CBP/p300, is Active in Preclinical Models of Androgen Receptor-Positive Breast Cancer. [Abstract]

2023 Mar;18(2):269-285. PMID: 36826464
Biomedicines

2026 May;14(5):949.
J Cell Commun Signal

Emerging role of HIC1 in prostate cancer progression and therapeutic response: A novel perspective. [Abstract]

2025 Oct 3;19(4):e12032. PMID: 41050263
Sci Rep

PACT is requisite for prostate cancer cell proliferation. [Abstract]

2025 Oct 21;15(1):36610. PMID: 41120564
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
J Biol Chem

The kinesin-14 family motor protein KIFC2 promotes prostate cancer progression by regulating p65. [Abstract]

2023 Nov;299(11):105253. PMID: 37716704
Sci Rep

Investigation of enzalutamide, docetaxel, and cabazitaxel resistance in the castration resistant prostate cancer cell line C4 using genome-wide CRISPR/Cas9 screening. [Abstract]

2023 Jun 3;13(1):9043. PMID: 37270558
Aging (Albany NY)

Preclinical studies show using enzalutamide is less effective in docetaxel-pretreated than in docetaxel-naïve prostate cancer cells. [Abstract]

2020 Sep 10;12(17):17694-17712. PMID: 32920545
Sci Rep

Drivers of AR indifferent anti-androgen resistance in prostate cancer cells. [Abstract]

2019 Sep 24;9(1):13786. PMID: 31551480
Sci Rep

Stress-induced tunneling nanotubes support treatment adaptation in prostate cancer. [Abstract]

2019 May 24;9(1):7826. PMID: 31127190
Sci Rep

Maintenance of MYC expression promotes de novo resistance to BET bromodomain inhibition in castration-resistant prostate cancer. [Abstract]

2019 Mar 7;9(1):3823. PMID: 30846826
Sci Rep

Galiellalactone inhibits the STAT3/AR signaling axis and suppresses Enzalutamide-resistant Prostate Cancer. [Abstract]

2018 Nov 23;8(1):17307. PMID: 30470788

Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. [Abstract]

Western analysis of protein expression in LNCaP and 16D CRPC cells treated with 10 μM ENZ for indicated days.

Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. [Abstract]

Protein expression analysis of p-STAT3S727, STAT3, PSA, AR and Vinculin in the treatment of ENZ and GPA500.
Sci Rep

Glucocorticoids Induce Stress Oncoproteins Associated with Therapy-Resistance in African American and European American Prostate Cancer Cells. [Abstract]

2018 Oct 10;8(1):15063. PMID: 30305646

Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Oct 10;8(1):15063. [Abstract]

The increased protein levels of both LEDGF/p75 and CLU are observed in cells treated with either 1 nM or 10 nM DHT, which is attenuated by exposure to 1 μM Enz.
J Endocrinol

Androgens modulate glucocorticoid receptor activity in adipose tissue and liver. [Abstract]

2019 Jan;240(1):51-63. PMID: 30400038

Enzalutamide purchased from MedChemExpress. Usage Cited in: J Endocrinol. 2019 Jan;240(1):51-63. [Abstract]

At the protein level, CORT-induced FKBP5 content in both WAT and liver is attenuated with AR antagonism.
J Biol Chem

Inhibition of cholesterol biosynthesis overcomes enzalutamide resistance in castration-resistant prostate cancer (CRPC). [Abstract]

2018 Sep 14;293(37):14328-14341. PMID: 30089652

Enzalutamide purchased from MedChemExpress. Usage Cited in: J Biol Chem. 2018 Sep 14;293(37):14328-14341. [Abstract]

C4-2R cells are treated with MK 733, Enzalutamide or combination of the two drugs at the indicated concentrations for 48 hours, followed by Immunoblotting (IB) against cleaved PARP.
Sci Rep

The Microwell-mesh: A high-throughput 3D prostate cancer spheroid and drug-testing platform. [Abstract]

2018 Jan 10;8(1):253. PMID: 29321576
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
Sci Rep

Aptamer-based Field-Effect Biosensor for Tenofovir Detection. [Abstract]

2017 Mar 15;7:44409. PMID: 28294122
Sci Rep

Bioluminescence Microscopy as a Method to Measure Single Cell Androgen Receptor Activity Heterogeneous Responses to Antiandrogens. [Abstract]

2016 Sep 28;6:33968. PMID: 27678181
J Pharm Sci

Characterization of CYP2C Induction in Cryopreserved Human Hepatocytes and Its Application in the Prediction of the Clinical Consequences of the Induction. [Abstract]

2018 Sep;107(9):2479-2488. PMID: 29802934
Am J Pathol

Testosterone-Induced H3K27 Deacetylation Participates in Granulosa Cell Proliferation Suppression and Pathogenesis of Polycystic Ovary Syndrome. [Abstract]

2024 Sep 5:S0002-9440(24)00331-6. PMID: 39243944
J Immunol

Restored Thymic Output after Androgen Blockade Participates in Antitumor Immunity. [Abstract]

2023 Feb 15;210(4):496-503. PMID: 36548468
Front Physiol

Transcriptional Repression and Protein Degradation of the Ca2+-Activated K+ Channel KCa1.1 by Androgen Receptor Inhibition in Human Breast Cancer Cells. [Abstract]

2018 Apr 16:9:312. PMID: 29713287

Enzalutamide purchased from MedChemExpress. Usage Cited in: Front Physiol. 2018 Apr 16:9:312. [Abstract]

Protein lysates of vehicle-, 1 μM BCT-, and 1 μM EZT-treated MDA-MB-453 cells are probed by immunoblotting with anti-K_Ca1.1 (upper panel) and anti-ACTB (lower panel) antibodies on the same filter.
EJNMMI Radiopharm Chem

Radiochemistry and comparative in vitro assessment of PSMA-617 labeled with lead-212 (212Pb), actinium-225 (225Ac), and lutetium-177 (177Lu). [Abstract]

2026 May 20. PMID: 42159963
Endocrinology

Androgen Receptors Promote Oxidative Phosphorylation and Resistance to Palmitate Lipotoxicity in ER-Mutant Breast Cancer. [Abstract]

2025 Dec 5;167(1):bqaf168. PMID: 41216931
Endocrinology

MED12 and CDK8/19 Modulate Androgen Receptor Activity and Enzalutamide Response in Prostate Cancer. [Abstract]

2024 Sep 10:bqae114. PMID: 39253786
Endocrinology

Insulin-Induced AKR1C3 Induces Fatty Acid Synthase in a Model of Human PCOS Adipocytes. [Abstract]

2023 Mar 13;164(5):bqad033. PMID: 36799021
Front Oncol

Huaier Extract Inhibits Prostate Cancer Growth via Targeting AR/AR-V7 Pathway. [Abstract]

2021 Feb 23;11:615568. PMID: 33708629
Arch Biochem Biophys

Chemical degrader enhances the treatment of androgen receptor-positive triple-negative breast cancer. [Abstract]

2022 May 30;721:109194. PMID: 35337811
Bioorg Med Chem

The splicing modulator sulfonamide indisulam reduces AR-V7 in prostate cancer cells. [Abstract]

2020 Oct 15;28(20):115712. PMID: 33069070
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
J Appl Toxicol

Biocompatibility and Toxicity Evaluation of an Elastin-Based Nanogel Carrier for Enzalutamide: Comprehensive Characterization, Controlled Release and Assessment in Zebrafish Embryos. [Abstract]

2026 Feb 8. PMID: 41655981
J Cancer Res Clin Oncol

Elevated VRK1 levels after androgen deprivation therapy promote prostate cancer progression by upregulating YAP1 expression. [Abstract]

2025 Mar 20;151(3):116. PMID: 40111564
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Mol Cell Biol

A Genome Wide CRISPR Screen Reveals That HOXA9 Promotes Enzalutamide Resistance in Prostate Cancer. [Abstract]

2024 Sep 20:1-14. PMID: 39300912
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SIRT5 suppresses the trophoblast cell proliferation, invasion, and migration to promote preeclampsia via desuccinylating HOXB3. [Abstract]

2024 Oct;41(10):2759-2770. PMID: 39145876
Mol Biol Cell

SPOP is essential for DNA-protein cross-link repair in prostate cancer cells: SPOP-dependent removal of topoisomerase 2A from the topoisomerase 2A-DNA cleavage complex. [Abstract]

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Cancer Genomics Proteomics

SCAMP3 and EPS8 Cooperatively Regulate EGFR Signaling to Promote Enzalutamide Resistance and Metastatic Potential in Prostate Cancer. [Abstract]

2025 Nov-Dec;22(6):953-970. PMID: 41151858
PLoS One

Combined AKT and MEK Pathway Blockade in Pre-Clinical Models of Enzalutamide-Resistant Prostate Cancer. [Abstract]

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Prostate

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

2025 Sep 19. PMID: 40968720
Prostate

PRMT5:MEP50 Are Mediators of Treatment-Induced Neuroendocrine Differentiation in Prostate Cancer. [Abstract]

2025 Sep;85(13):1196-1207. PMID: 40677010
Prostate

Androgen receptor and MYC transcriptomes are equilibrated in multilayer regulatory circuitries in prostate cancer. [Abstract]

2023 Nov;83(15):1415-1429. PMID: 37565264
Prostate

Diptoindonesin G antagonizes AR signaling and enhances the efficacy of antiandrogen therapy in prostate cancer. [Abstract]

2022 Jun;82(8):917-932. PMID: 35322879
Prostate

NPRL2 enhances autophagy and the resistance to Everolimus in castration-resistant prostate cancer. [Abstract]

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Dig Dis Sci

Androgen Signaling in Esophageal Adenocarcinoma Cell Lines In Vitro. [Abstract]

2017 Dec;62(12):3402-3414. PMID: 29052817
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Suppression of LIM and SH3 Domain Protein 1 (LASP1) Negatively Regulated by Androgen Receptor Delays Castration Resistant Prostate Cancer Progression. [Abstract]

2017 Feb;77(3):309-320. PMID: 27775154

Enzalutamide purchased from MedChemExpress. Usage Cited in: Prostate. 2017 Feb;77(3):309-320. [Abstract]

LNCaP cell are treated with 20 mM LY294002 or 10 mM U0126 for 1 hr before 10 mM of ENZ. Whole-cell extracts are subjected to SDS–PAGE, followed by western blot analysis for the indicated proteins.
Prostate

Generation of a C57BL/6 MYC-Driven Mouse Model and Cell Line of Prostate Cancer. [Abstract]

2016 Sep;76(13):1192-202. PMID: 27225803
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Next-generation steroidogenesis inhibitors, dutasteride and abiraterone, attenuate but still do not eliminate androgen biosynthesis in 22RV1 cells in vitro. [Abstract]

2014 Oct;144 Pt B:436-44. PMID: 25201454
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Stevia eupatoria and Stevia pilosa Extracts Inhibit the Proliferation and Migration of Prostate Cancer Cells. [Abstract]

2020 Feb 23;56(2):90. PMID: 32102219
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TP53 loss-of-function causes vulnerability to autophagy inhibition in aggressive prostate cancer. [Abstract]

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Androgen Deprivation-Induced TET2 Activation Fuels Prostate Cancer Progression via Epigenetic Priming and Slow-Cycling Cancer Cells. [Abstract]

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Patent

US20180305771A1.
Oncotarget

YAP1 regulates prostate cancer stem cell-like characteristics to promote castration resistant growth. [Abstract]

2017 Dec 7;8(70):115054-115067. PMID: 29383141

Enzalutamide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2017 Dec 7;8(70):115054-115067. [Abstract]

The levels of YAP1 protein are measured in LNCaP cells treated for 24 h with the AR antagonist MDV3100 (Enzalutamide, 100 nM) and ICI 176334 (10 mM).
University of British Columbia

2017 Dec.

Enzalutamide purchased from MedChemExpress. Usage Cited in: University of British Columbia. 2017 Dec.

p-TNIK (S764), T-TNIK, and PSA protein expression are assessed in (A) LNCaP and 16D^CRPC cells that are treated with 10 μM Enzalutamide (ENZ) in media containing 10% FBS for 2, 4, and 7 days by western blot. Vinculin is used as loading control.
University of British Columbia

2017 Dec.
J Oncol Res Ther

2017 (03), ISSN: 2574-710X.
Oncotarget

Integrative molecular network analysis identifies emergent enzalutamide resistance mechanisms in prostate cancer. [Abstract]

2017 Nov 20;8(67):111084-111095. PMID: 29340039
Horm Cancer

Role of 20-Hydroxyeicosatetraenoic Acid (20-HETE) in Androgen-Mediated Cell Viability in Prostate Cancer Cells. [Abstract]

2017 Aug;8(4):243-256. PMID: 28639228

Enzalutamide purchased from MedChemExpress. Usage Cited in: Horm Cancer. 2017 Aug;8(4):243-256. [Abstract]

LNCaP cells are grown in complete media for 24 h in the presence of vehicle (control) or Enzalutamide, 10 μM, and protein expression normalized to β-tubulin.
Oncotarget

Beta-catenin represses protein kinase D1 gene expression by non-canonical pathway through MYC/MAX transcription complex in prostate cancer. [Abstract]

2017 Aug 12;8(45):78811-78824. PMID: 29108267
University of British Columbia

2017 Apr.

Enzalutamide purchased from MedChemExpress. Usage Cited in: University of British Columbia. 2017 Apr.

VCaP (mock) and VCaP (UGT2B17) cells are cultured in the RPMI1640 medium plus 5% CSS. Cells are treated with vehicle, 10 nM of R1881 or 10 μM of Enzalutamide (ENZ) for 0 or 28 days. Protein levels of UGT2B17, pSrc, tSrc, pAKT, total AKT, pSTAT3, total STAT3, pSTAT5, total STAT5 and β-actin are determined by immunoblotting.
Oncotarget

Critical role of androgen receptor level in prostate cancer cell resistance to new generation antiandrogen enzalutamide. [Abstract]

2016 Sep 13;7(37):59781-59794. PMID: 27486973

Enzalutamide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Sep 13;7(37):59781-59794. [Abstract]

Short term treatment (14 days) of LAPC4 vehicle cells with 8μM Enzalutamide clearly demonstrates that AR overexpression is not a short term effect of drug treatment but develops as a long term adaptation during acquisition of resistance. It has been suggested that presence of a truncated AR variant (AR-V7) is associated with resistance to Enzalutamide.
University of California

2016 Aug.
Oncotarget

Cellular androgen content influences enzalutamide agonism of F877L mutant androgen receptor. [Abstract]

2016 Jun 28;7(26):40690-40703. PMID: 27276681

Enzalutamide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2016 Jun 28;7(26):40690-40703. [Abstract]

DHT alone, Enzalutamide alone, or the combination in androgen-depleted conditions also increase expression of canonical AR targets: KLK3, TMPRSS2, and NKX3.1 and increase protein levels of PSA encoded by the KLK3 gene.
Oncotarget

Catalytic inhibitors of DNA topoisomerase II suppress the androgen receptor signaling and prostate cancer progression. [Abstract]

2015 Aug 21;6(24):20474-84. PMID: 26009876

Enzalutamide purchased from MedChemExpress. Usage Cited in: Oncotarget. 2015 Aug 21;6(24):20474-84. [Abstract]

LNCaP cells are cultured in RPMI1640 medium containing 5% CSS and treated with vehicle, 1 μM of ICRF187 or 1 μM of ICRF193 in addition to vehicle, 10 nM of R1881 or 10 μM of ENZ treatment for 2 hours. Three independent ChIP experiments are performed using the AR antibody. AR protein levels under 2 and 24 hour treatment are detected by Western blotting.
Oncotarget

A novel calcium-dependent mechanism of acquired resistance to IGF-1 receptor inhibition in prostate cancer cells. [Abstract]

2014 Oct 15;5(19):9007-21. PMID: 25344862
Patent

US20140088178A1.

Enzalutamide purchased from MedChemExpress. Usage Cited in: Patent. US20140088178A1.

Effect of AR1 (MDV-3100) administration on AKT and ERK phosphorylation and protein levels in LNCaP cells. (A), 10 μM AR1. (B), after 48 hours of AR1 treatment at indicated concentrations. (C), Dose dependent change of expression level of AKT or ERK after treatment with AR1. (D), Dose dependent change of expression level of AKT or ERK after treatment with AR1.
Annual rept

15 Sep 2012-14 Sep 2013

Solvent & Solubility

In Vitro:

DMSO : ≥ 50 mg/mL (107.66 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

2.1531 mL

10.7657 mL

21.5313 mL

5 mM

0.4306 mL

2.1531 mL

4.3063 mL

10 mM

0.2153 mL

1.0766 mL

2.1531 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Molarity Calculator

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

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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 (5.38 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% Corn Oil

Solubility: ≥ 2.5 mg/mL (5.38 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.

Protocol 3

Add each solvent one by one: 5% DMSO 40% PEG300 5% Tween-80 50% Saline

Solubility: 2.5 mg/mL (5.38 mM); Suspended solution; Need ultrasonic

Working Solution

For the following dissolution methods, please prepare the working solution directly:

It is recommended to prepare fresh solutions and use them promptly within a short period of time.

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: 1% Tween-80 in PBS

Solubility: 10 mg/mL (21.53 mM); Suspended solution; Need ultrasonic and warming and heat to 60°C

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

Protocol

Cell Assay^[1]

LNCaP cells (10⁷ cells/condition) are grown in RPMI media supplemented with 5% charcoalstripped serum for 22 days, then treated with DMSO or 1 nM R1881, combined with an antiandrogen (DMSO, 1 μM ICI 176334, 10 μM ICI 176334, 1 μM RD162, 10 μM RD162, 1 μM MDV3100, or 10 μM MDV3100) for 8 hours. An aliquot of cells are harvested for qRT-PCR of PSA and TMPRSS2 mRNA. The remaining cells are cross-linked using 1% paraformaldehyde for 10 minutes, then glycine is added and samples centrifuged (4°C, 4000 rpm, 5 minutes) to stop further crosslinking. Chromatin immunoprecipitation is performed using a chromatin immunoprecipitation assay kit. Immunoprecipitated DNA is amplified by real-time PCR. Primers are PSA enhancer forward-ATGTTCACATTAGTACACCTTGCC and reverse-TCTCAGATCCAGGCTTGCTTACTGTC and TMPRSS2 enhancer forward-TGGTCCTGGATGATAAAAAAAGTTT and reverse-GACATACGCCCCACAACAGA^[1].

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

Animal Administration^[3]^[4]

Mice^[3]
Following a 5-day acclimation period, 5- to 9-week-old male CB17SCID mice are castrated and allowed to recover for an additional 5 days before inoculation with tumor cells. LNCaP cells co-expressing exogenous AR and the AR-dependent reporter construct ARR2-Pb-Luc (LNCaP-AR-Lux cells) are used to generate a xenograft model of human prostate cancer. Before implantation, LNCaP-AR-Lux cells are prepared by the addition of trypsin-EDTA, washed with complete medium, collected and resuspended at 20×10⁶ cells/mL. Cell suspensions are diluted with Matrigel to 2×10⁶ cells/0.2 mL and delivered subcutaneously in the suprascapular region. Tumor growth is monitored to the volume of 100 mm³ when treatment begins (80 days). The observed rate of tumor take with LNCaP-AR-Lux cells is between 70% and 80%. Body weight and tumor volumes (width²×length/2) are measured two to three times per week with a digital caliper, and the average tumor volumes are determined. Test drugs are diluted in Tween 80:PEG 400, and stored at 4°C until administration by oral gavage. Each group of mice (n=7) is treated daily for 28 consecutive days with 1, 10, or 50 mg/kg Enzalutamide, vehicle control, or 50 mg/kg ICI 176334. At the end of the treatment period or when tumor volume exceeded 1,000 mm³, animals are euthanized and blood and tissue samples are collected for analysis.
Rats^[4]
Male SD rats (n=3) are administered Enzalutamide through the tail vein (intravenous) and by oral gavage at 1 mg/kg and are kept in metabolic cages after dosing. Urine and feces samples are collected over the following time intervals after dosing: 0-2, 2-4, 4-6, 6-10, 10-24, 24-48, and 48-72 h. The metabolic cages are rinsed with distilled water, and residues are added to the urine samples at 72 h. To extract the Enzalutamide present in the feces, samples are shaken vigorously for 12 h with 50 % methanol.

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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (394 KB)
- English - EN (394 KB)
- Français - FR (394 KB)
- Deutsch - DE (394 KB)
- Norwegian - NO (394 KB)
- Español - ES (394 KB)
- Swedish - SV (394 KB)
- Italian - IT (394 KB)
- Portuguese - PT (394 KB)
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)
Handling Instructions (2659 KB)

References

[1]. Tran C, et al. Development of a second-generation antiandrogen for treatment of advanced prostate cancer. Science, 2009, 324 (5928), 787-790. [Content Brief]

[2]. Scher HI, et al. Antitumour activity of MDV3100 in castration-resistant prostate cancer: a phase 1-2 study. Lancet, 2010, 375(9724), 1437-1446. [Content Brief]

[3]. Guerrero J, et al. Enzalutamide, an androgen receptor signaling inhibitor, induces tumor regression in a mouse model of castration-resistant prostate cancer. Prostate. 2013 Sep;73(12):1291-305. [Content Brief]

[4]. Kim TH, et al. Pharmacokinetics of enzalutamide, an anti-prostate cancer drug, in rats. Arch Pharm Res. 2015 Nov;38(11):2076-82. [Content Brief]

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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.1531 mL	10.7657 mL	21.5313 mL	53.8283 mL
	5 mM	0.4306 mL	2.1531 mL	4.3063 mL	10.7657 mL
	10 mM	0.2153 mL	1.0766 mL	2.1531 mL	5.3828 mL
	15 mM	0.1435 mL	0.7177 mL	1.4354 mL	3.5886 mL
	20 mM	0.1077 mL	0.5383 mL	1.0766 mL	2.6914 mL
	25 mM	0.0861 mL	0.4306 mL	0.8613 mL	2.1531 mL
	30 mM	0.0718 mL	0.3589 mL	0.7177 mL	1.7943 mL
	40 mM	0.0538 mL	0.2691 mL	0.5383 mL	1.3457 mL
	50 mM	0.0431 mL	0.2153 mL	0.4306 mL	1.0766 mL
	60 mM	0.0359 mL	0.1794 mL	0.3589 mL	0.8971 mL
	80 mM	0.0269 mL	0.1346 mL	0.2691 mL	0.6729 mL
	100 mM	0.0215 mL	0.1077 mL	0.2153 mL	0.5383 mL

Keywords

Enzalutamide

220 Cited Publications

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Enzalutamide

Anti-Infection Compound Library

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Autophagy Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Targeted Therapy Drug Library

Transcription Factor-Targeted Library

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Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

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Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

RNA Binding Bioactive Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Enzalutamide

Biological Activity

Chemical Information

Publications (220)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Enzalutamide

Anti-Infection Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Autophagy Compound Library

Drug Repurposing Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Anti-Pancreatic Cancer Compound Library

Targeted Therapy Drug Library

Transcription Factor-Targeted Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Prostate Cancer Compound Library

Nuclear Receptor Compound Library

Heterocyclic Compound Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Anti-Cancer Approved Drug Library

Mass Spectrometry Human Metabolite Library

Cardiotoxic Compound Library

RNA Binding Bioactive Compound Library

Classic FDA-Approved Drug Library

Publications Citing Use of MedChemExpress (MCE) Enzalutamide

Biological Activity

Chemical Information

Publications (220)

Solvent & Solubility

Protocol

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Enzalutamide Related Classifications

Cat. No.: HY-70002