Enzalutamide (MDV3100)

For research use only.

Catalog No.S1250

302 publications

Enzalutamide (MDV3100) Chemical Structure

CAS No. 915087-33-1

Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.

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Selleck's Enzalutamide (MDV3100) has been cited by 302 publications

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Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells. Enzalutamide is shown to increase autophagy.
Androgen Receptor [1]
(LNCaP cells)
36 nM
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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
human LNCAP NXrGXG1oS3m2b4TvfIlkKEG|c3H5 MXu3JIRigXN? MoWzPVUmKEW2T1i= NYDNXJR7UUN3ME21MlEzKM7:TR?= MWqyN|cyOzV4Nx?=
human LNCAP Mle5SpVv[3Srb36gRZN{[Xl? MX6xJO69VQ>? NFHBfYxFVVOR MnvHTY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7N MkT5NlAzOTh5MUe=
VCaP MVvGeY5kfGmxbjDBd5NigQ>? MoLpNVAh|ryP NEDj[ZozPCCq Mn36SG1UVw>? Ml;yV5VxeHKnc4Pld{BtcWejbnStcYVlcWG2ZXSgRXIuTkxic3nncoFtcW6pIB?= NW\QWoR1OjJ5MUC0N|Y>
BCK4 NWT1VXA{TnWwY4Tpc44hSXO|YYm= MlnPNVAh|ryP MVm3JIRigXN? NX;yWI5yTE2VTx?= MUjJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? NEXRfpUzPDR3MUGwPS=>
MCF7s MV\GeY5kfGmxbjDBd5NigQ>? M2rTR|ExKM7:TR?= NVHReVg5PiCmYYnz NGnDPHBFVVOR NILyOmdKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= M{jFflI1PDVzMUC5
PC-3 MX3GeY5kfGmxbjDBd5NigQ>? NIXDVJEyOCEQvF2= NFrqWWE4OiCq MVPEUXNQ MUPEc4V{KG6xdDDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?= NX3KW|d4OjV|NES4OlQ>

... Click to View More Cell Line Experimental Data

Methods Test Index PMID
Western blot
AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7; 

PubMed: 28607007     

Treatment of VCaP cells with NOTCH inhibitor, GSI-1, in combination with Enzalutamide (Enz) augmentes its effects on the inhibition of AR, ERG, PSA, NOTCH1 and NOTCH2 expression and induces cleavage of PARP1 and Caspase 7

AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166); 

PubMed: 26378044     

LNCaP95 (LN95) cells were maintained in medium containing 5% CSS and then treated with 5μM of enzalutamide (ENZ) for 0-24 hours. Whole cell lyses were extracted. AR-FL, AR-v7, phosphor-AR(ser213), phosphorAkt(ser473), total Akt, total PP-1, phosphor-Mdm2(ser166), total Mdm2 and β-actin were measured by immunoblotting.


PubMed: 29277895     

Western blotting is used to analyze CXCR7 protein levels in VCaP and C4-2B cells.

28607007 26378044 29277895
Growth inhibition assay
Cell proliferation; 

PubMed: 28115200     

Proliferation of the LNCaP prostate cancer cell line, the Ramos Burkitt's cell line, and the Granta, Jeko-1, Rec-1 and Maver-1 MCL cell lines plated in charcoal stripped serum for 96 hours in the absence or presence of enzalutamide (10uM). Data are representative of 3 independent experiments.


PubMed: 27588408     

Representative immunofluorescent images show the expression and subcellular localization of AR in 22Rv1 cells overexpressing PIP5K1α that were treated with vehicle control, enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B.


PubMed: 27588408     

Representative immunofluorescent images of subcellular localization of pAKT S473 expression in PC3 cells expressing AR-V7 that were treated with vehicle control (Ctrl), enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B (ENZ+ISA2011B). The cancer cells are indicated by the arrows.


PubMed: 29277895     

Immunofluorescence staining is used to analyze CXCR7 protein levels in prostate cancer cells.

27588408 29277895

PubMed: 27015557     

MDA-MB-231 cells were treated with 10 μM enzalutamide or vehicle for 48 hours. Levels of OPG (osteoprotegerin) in the supernatant of MDA-MB-231 cells as determined by ELISA. Data are representative of 2 independent experiments.

In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]


Kinase Assay:[3]
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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:[1]
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  • 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.
    (Only for Reference)
Animal Research:[1]
- Collapse
  • Animal Models: Castration-resistant LNCaP/HR xenografts in male SCID mice
  • Dosages: 10 mg/kg
  • Administration: Administered via gavage daily
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 92 mg/mL warmed (198.08 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 464.44


CAS No. 915087-33-1
Storage powder
in solvent
Synonyms N/A
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04335682 Not yet recruiting Drug: Darolutamide|Drug: Enzalutamide Metastatic Prostate Cancer|Prostate Cancer Metastatic|Prostate Cancer|Castrate Resistant Prostate Cancer Alliance Foundation Trials LLC.|Bayer August 2020 Phase 2
NCT04456049 Not yet recruiting Drug: Enzalutamide COVID-19 Infection Ricardo Pereira Mestre|Oncology Institute of Southern Switzerland|Institute of Oncology Research|Institute for Research in Biomedicine|Ente Ospedaliero Cantonale Bellinzona July 2020 Phase 2
NCT04443062 Recruiting Drug: 177Lu-PSMA-I&T Prostate Cancer Radboud University|Prostaatkankerstichting July 20 2020 Phase 2

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Frequently Asked Questions

  • Question 1:

    I would like to inquire about the usage or solubility of S1250, Enzalutamide.

  • Answer:

    For in vivo experiment, S1250 can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5mg/ml as a suspension for oral gavage. And it can be dissolved in 15% DMSO+85% PEG 300 at 10mg/ml as a clear solution. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID