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Reagents and instruments for immunology, cell biology and molecular biology.

Enzalutamide [915087-33-1]

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Cat# HY-70002-10mg

Size : 10mg

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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	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	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	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	>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	>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	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	>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]
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	>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	>1 μM 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	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	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	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	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: 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: 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	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	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	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	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 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: 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	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	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	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	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	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	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]
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	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	>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	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	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	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: 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	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	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	44.6 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]
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	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	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	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]
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	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	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	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	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	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	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	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	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	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	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: 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	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: 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	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	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	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	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	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	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	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	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	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	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	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	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	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	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	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	36 nM Compound: 68	Antiproliferative activity against human LNCaP cells Antiproliferative activity against human LNCaP cells	[PMID: 35786895]
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	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	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	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	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	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	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	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	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	18 μM Compound: Enz	Cytotoxicity against human C42B cells Cytotoxicity against human C42B cells	[PMID: 34225450]
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	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]
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]
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	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	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	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	>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	>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	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	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	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]
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	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]
RWPE-1	IC₅₀	>40 μM Compound: Enz	Cytotoxicity against human RWPE-1 cells Cytotoxicity against human RWPE-1 cells	[PMID: 34225450]
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	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	>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	>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	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	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	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	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	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	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	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	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	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	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: 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	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	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.

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.

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

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

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 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.

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

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

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.38 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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

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

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

Purity & Documentation

Purity: 99.97%

Data Sheet (282 KB) SDS (394 KB)

COA (251 KB) HNMR (279 KB) RP-HPLC (222 KB) LCMS (93 KB) Elemental Analysis Report (108 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]

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