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

Enzalutamide

Synonyms: MDV3100

Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.

Enzalutamide Chemical Structure

Enzalutamide Chemical Structure

CAS: 915087-33-1

Selleck's Enzalutamide has been cited by 482 publications

Purity & Quality Control

Batch: Purity: 99.99%
99.99

Products often used together with Enzalutamide

Apalutamide (ARN-509)

Enzalutamide and Apalutamide improve metastasis-free survival (MFS) and overall survival in patients with non-metastatic castration-resistant prostate cancer (M0CRPC).

Swami U, et al. Cancer Treat Res Commun. 2020;25:100205.

Darolutamide (ODM-201)

Enzalutamide and Darolutamide improve metastasis-free survival (MFS) and overall survival in patients with non-metastatic castration-resistant prostate cancer (M0CRPC).

Swami U, et al. Cancer Treat Res Commun. 2020;25:100205.

Bicalutamide

Enzalutamide outperforms Bicalutamide in median progression-free survival (PFS) in patients with metastatic castration-resistant prostate cancer.

Shore ND, et al. Lancet Oncol. 2016;17(2):153-163.

Abiraterone

Enzalutamide and Abiraterone prolong progression-free survival (PFS) and overall survival (OS) in patients with metastatic castration-resistant prostate cancer.

Wang Y, et al. J Cancer Res Clin Oncol. 2018;144(9):1751-1768.

Abiraterone Acetate

Enzalutamide and Abiraterone acetate are second-generation anti-androgens that improve survival in patients with castration-resistant prostate cancer (CRPC).

Moreira-Silva F, et al. Front Oncol. 2022 May 24;12:877379.

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Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP Cytotoxic Assay 7 days 95% EtOH IC50=5.12 μM 23713567
human LNCAP Function Assay 1 μM DMSO Inhibits prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 100-1000nM 20218717
VCaP Function Assay 10 μM 24 h DMSO Suppresses ligand-mediated AR-FL signaling 22710436
BCK4 Function Assay 10 μM 7 days DMSO Inhibits estradiol-mediated proliferation 24451109
MCF7s Function Assay 10 μM 6 days DMSO Inhibits estradiol-mediated proliferation 24451109
PC-3 Function Assay 10 μM 72 h DMSO Does not inhibit cell proliferation 25344864
CWR22Rv1 Function Assay 15 μM 24 h DMSO Does not affect the full length AR expression 23713567
LNCAP/AR Antagonist activity assay IC50 = 0.021 μM 27717544
MDA-MB-453 Antagonist activity assay EC50 = 0.049 μM 23713567
LNCAP Antagonist activity assay 72 h IC50 = 0.05 μM 30193215
LNCAP Antagonist activity assay 72 h IC50 = 0.09 μM 30193215
LNCAP Growth inhibition assay GI50 = 0.12 μM 28011219
LNCAP Antiproliferative activity assay 3 days IC50 = 0.1271 μM 26046313
LNCAP Antagonist activity assay 6 days GI50 = 0.29 μM 28011219
UAS-bla GripTite 293 Antagonist activity assay 16 to 24 h IC50 = 0.361 μM 27301368
mammalian expression system Antagonist activity assay 22 to 24 h EC50 = 0.42 μM 28385503
VCaP Growth inhibition assay 144 h GI50 = 0.61 μM 25121586
LNCaP Antagonist activity assay 2 h EC50 = 0.915 μM 23713567
COS7 Antagonist activity assay 24 h IC50 = 1.26 μM 29117897
AR LBD mutant Antagonist activity assay 4 h IC50 = 1.35 μM 27810589
LNCAP Growth inhibition assay GI50 = 2.88 μM 25634130
CWR22Rv1 Growth inhibition assay GI50 = 3.34 μM 25634130
LNCAP Cytotoxicity assay 7 days GI50 = 5.12 μM 23713567
PC3 Growth inhibition assay GI50 = 9.15 μM 25634130
CWR22Rv1 Cell survival assay 144 h IC50 = 9.7 μM 25121586
LNCAP Antiproliferative activity assay 96 h IC50 = 11.47 μM 27301368
LNCaP-hr Antiproliferative activity assay 3 days IC50 = 12.5 μM 27810589
LNCAP Antiproliferative activity assay 3 days IC50 = 12.5 μM 29117897
LNCaP Antagonist activity assay 144 h GI50 = 18.88 μM 28272894
LNCaP-AR Growth inhibition assay 144 h GI50 = 18.9 μM 25121586
C4-2B Antiproliferative activity assay 12 h IC50 = 20.77 μM 29758518
A31 Growth inhibition assay 72 h GI50 = 27.5 μM 28011219
22Rv1 Antiproliferative activity assay 96 h IC50 = 31.76 μM 27301368
22Rv1 Antiproliferative activity assay 96 h IC50 = 31.76 μM 26965862
DU145 Antiproliferative activity assay 96 h IC50 = 32.27 μM 27301368
LNCAP Antiproliferative activity assay 72 h IC50 = 33.84 μM 29448139
CW22Rv1 Antagonist activity assay 72 h IC50 = 35.75 μM 28272894
22Rv1 Antiproliferative activity assay 72 h IC50 = 36.66 μM 29448139
22Rv1 Antiproliferative activity assay 12 h IC50 = 36.66 μM 29758518
LNCAP Antiproliferative activity assay 12 h IC50 = 42.37 μM 29758518
DU145 Antiproliferative activity assay 3 days IC50 = 46.1 μM 27810589
DU145 Antiproliferative activity assay 3 days IC50 = 46.1 μM 29117897
Click to View More Cell Line Experimental Data

Biological Activity

Description Enzalutamide is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Targets
Androgen Receptor [1]
(LNCaP cells)
36 nM
In vitro
In vitro Enzalutamide has greater affinity to AR than Bicalutamide 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 could inhibit 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]
Kinase Assay AR reporter assay
Enzalutamide is evaluated by an artificial AR response reporter system in a hormone refractory prostate cancer cell line. In this system, the prostate cancer LNCaP cells are engineered to stably express about 5-fold higher level of AR than endogenous level. The exogenous AR has similar properties to endogenous AR in that both are stabilized by a synthetic androgen R1881. The AR-over expressed cells are also engineered to stably incorporate an AR response reporter and the reporter activity of these cells shows features of hormone refractory prostate cancer. The antagonistic activity of Enzalutamide is tested in the presence of 100 pM of R1881. Engineered LNCaP cells are maintained in Iscove's medium containing 10% fetal bovine serum (FBS). Two days prior to Enzalutamide treatment, the cells are grown in Iscove's medium containing 10% charcoal-stripped FBS (CS-FBS) to deprive of androgens. The cells are split and grown in Iscove's medium containing 10% CS-FBS with 100 pM of R1881 and increasing concentrations of Enzalutamide. After two days of incubation, reporter activities are assayed.
Cell Research Cell lines LNCaP or LNCaP/AR cells
Concentrations 0-10 μM
Incubation Time 1-4 days
Method Enzalutamide is diluted in DMSO. LNCaP or LNCaP/AR cells (104 cells/well) are androgen-starved by growth in media containing 5-10% charcoal-stripped serum for 3-5 days. Then the cells are challenged with various concentrations of Enzalutamide in media containing 5-10% charcoal-stripped serum.
Experimental Result Images Methods Biomarkers Images PMID
Western blot AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7 AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166) CXCR7 28607007
Growth inhibition assay Cell proliferation 28115200
Immunofluorescence AR pAKT(S473) CXCR7 27588408
ELISA osteoprotegerin 27015557
In Vivo
In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]
Animal Research Animal Models Castration-resistant LNCaP/HR xenografts in male SCID mice
Dosages 10 mg/kg
Administration Administered via gavage daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05339672 Recruiting Drug-drug Interaction Radboud University Medical Center|Astellas Pharma Inc July 1 2024 --
NCT06130995 Not yet recruiting Androgen Deprivation Therapy|Locally Advanced Prostate Cancer University of Oklahoma January 2024 Phase 1
NCT06096870 Not yet recruiting Prostate Cancer|Recurrent Prostate Cancer|PET Positive National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) January 12 2024 Phase 2
NCT05743621 Not yet recruiting Prostatic Neoplasms Castration-Resistant Weill Medical College of Cornell University|Sagimet Biosciences Inc. April 2023 Phase 1

Chemical lnformation & Solubility

Molecular Weight 464.44 Formula

C21H16F4N4O2S
CAS No. 915087-33-1 SDF Download Enzalutamide SDF
Smiles CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 92 mg/mL ( (198.08 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 24 mg/mL

Water : Insoluble


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