Enzalutamide (MDV3100)

Catalog No.S1250

Enzalutamide (MDV3100) Chemical Structure

Molecular Weight(MW): 464.44

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

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In DMSO USD 300 In stock
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USD 270 In stock
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Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
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 M2rXNGN6fG:2b4jpZ{BCe3OjeR?= MoDLO{Bl[Xm| NFrkPJM6PSViRYTPTC=> M4DLW2lEPTB;NT6xNkDPxE1? M4\rRVI{PzF|NU[3
human LNCAP NVvWVpZkTnWwY4Tpc44hSXO|YYm= M{fRRVEh|ryP M{\5W2ROW09? MUDJcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2= MVSyNFIyQDdzNx?=
VCaP M1TtdmZ2dmO2aX;uJGF{e2G7 NIr5PHcyOCEQvF2= NFjDNWYzPCCq NGW2THdFVVOR NHqzfZVUfXCycnXzd4V{KGyrZ3Hu[E1u\WSrYYTl[EBCWi2ITDDzbYdv[Wyrbneg Mn:4NlI4OTB2M{[=
BCK4 MUnGeY5kfGmxbjDBd5NigQ>? NF3EZYMyOCEQvF2= MX:3JIRigXN? MnrISG1UVw>? NXT1WXR5UW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= M3LoOlI1PDVzMUC5
MCF7s M2W2SWZ2dmO2aX;uJGF{e2G7 MknONVAh|ryP NHqyVYk3KGSjeYO= MoT2SG1UVw>? MUjJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? MVSyOFQ2OTFyOR?=
PC-3 Mn3FSpVv[3Srb36gRZN{[Xl? NVnZWlQyOTBizszN NYTDbo5nPzJiaB?= NFOwOGxFVVOR MnPZSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= MknaNlU{PDR6NkS=
CWR22Rv1 MkHDSpVv[3Srb36gRZN{[Xl? NID5N5oyPSEQvF2= MWiyOEBp NFfKc2VFVVOR MX;Ec4V{KG6xdDDh[oZm[3RidHjlJIZ2dGxibHXu[5RpKEGUIHX4dJJme3Orb36= NIP2eYszOzdzM{W2Oy=>

... Click to View More Cell Line Experimental Data

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]
+ Expand

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]
+ Expand
  • 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]
+ Expand
  • Animal Models: Castration-resistant LNCaP/HR xenografts in male SCID mice
  • Formulation: Formulated in 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO
  • 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
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+1% CMC Na+1% Tween-80
For best results, use promptly after mixing.

* 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

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT03123978 Recruiting Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Cancer University of California Davis|National Cancer Institute (NCI)|Pandomedx January 9 2017 Phase 1
NCT02528643 Active not recruiting Advanced Hepatocellular Carcinoma Astellas Pharma Global Development Inc.|Pfizer|Astellas Pharma Inc November 9 2015 Phase 2
NCT02485691 Recruiting Prostate Cancer Metastatic Sanofi November 9 2015 Phase 4
NCT01650194 Completed Metastatic Castration-Resistant Prostate Cancer Astellas Pharma Global Development Inc.|Medivation Inc.|Astellas Pharma Inc July 9 2012 Phase 2
NCT02607228 Active not recruiting Metastatic Castrate-Resistant Prostate Cancer Gilead Sciences December 8 2015 Phase 1|Phase 2
NCT02495974 Active not recruiting Metastatic Castration Resistant Prostate Cancer Astellas Pharma Europe Ltd.|Medivation Inc.|Astellas Pharma Inc September 8 2015 --

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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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