Enzalutamide (MDV3100)

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

Price Stock Quantity  
USD 300 In stock
USD 150 In stock
USD 270 In stock
USD 770 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Enzalutamide (MDV3100) Chemical Structure

Enzalutamide (MDV3100) Chemical Structure
Molecular Weight: 464.44

Validation & Quality Control

Customer Product Validation(3)

Quality Control & MSDS

Related Compound Libraries

Enzalutamide (MDV3100) is available in the following compound libraries:

Androgen Receptor Inhibitors with Unique Features

  • Selective AR Agonist

    Andarine Selective non-steroidal AR agonist, Ki=4 nM.

  • Most Potent AR Antagonist

    ARN-509 Androgen receptor, IC50=16 nM.

  • FDA-approved AR Antagonist

    Bicalutamide Approved by FDA for prostate cancer.

  • Newest AR Antagonist

    AZD3514 Potent and oral androgen receptor downregulator with Ki of 2.2 μM.

Product Information

  • Compare Androgen Receptor Chemicals
    Compare Androgen Receptor Products
  • Research Area

Product Description

Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM in LNCaP cells.
Targets Androgen Receptor [1]
(LNCaP cells)
IC50 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 LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
human LNCAPMnG0SpVv[3Srb36gRZN{[Xl?NVW3ZpQ{OSEQvF2=MVPEUXNQMnX1TY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7NNXmwOld[OjB{MUi3NVc>

... 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]

Protocol(Only for Reference)

Kinase Assay: [3]

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 Assay: [1]

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.

Animal Study: [1]

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

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)


[1] Tran C, et al, Science, 2009, 324 (5928), 787-790.

[2] Scher HI, et al, Lancet, 2010, 375(9724), 1437-1446.

view more

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-11-14)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02491411 Not yet recruiting Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Prostate Adenocarcinoma|Stage IV Prostate Cancer Sidney Kimmel Comprehensive Cancer Center|National Cancer  ...more Sidney Kimmel Comprehensive Cancer Center|National Cancer Institute (NCI) December 2015 --
NCT02384382 Recruiting Prostate Carcinoma Metastatic to the Bone|Castration Resistant Prostate Cancer Medivation, Inc.|Astellas Pharma Inc November 2015 Phase 2
NCT02532114 Not yet recruiting Hormone-Resistant Prostate Cancer|Metastatic Prostate Carcinoma|Recurrent Prostate Carcinoma|Stage IV Prostate Adenocarcinoma University of Washington|National Cancer Institute (NCI) November 2015 Phase 1
NCT02528643 Not yet recruiting Advanced Hepatocellular Carcinoma Astellas Pharma Global Development, Inc.|Medivation, Inc.  ...more Astellas Pharma Global Development, Inc.|Medivation, Inc.|Astellas Pharma Inc October 2015 Phase 2
NCT02380313 Not yet recruiting Cancer GlaxoSmithKline October 2015 Phase 1

view more

Chemical Information

Download Enzalutamide (MDV3100) SDF
Molecular Weight (MW) 464.44


CAS No. 915087-33-1
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 92 mg/mL warmed (198.08 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 2% DMSO/30% PEG300 5 mg/mL
* <1 mg/ml means slightly soluble or 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 Name  4-​[3-​[4-​cyano-​3-​(trifluoromethyl)​phenyl]​-​5,​5-​dimethyl-​4-​oxo-​2-​thioxo-​1-​imidazolidinyl]​-​2-​fluoro-​N-​methyl-benzamide

Customer Product Validation (3)

Click to enlarge
Source Cancer Sci 2013 104(8), 1027-32. Enzalutamide (MDV3100) purchased from Selleck
Method Transfection and luciferase activity assay
Cell Lines Tramp-C1, PTENCaP8 cells
Incubation Time 48 h
Results When bicalutamide and MDV3100were used to block AR, BMP-6 no longer increased the probasin promoter activity in Tramp-C1 and PTENCaP8 whenRAW 264.7 cells were present.

Click to enlarge
Source PLoS One 2013 8, e53701. Enzalutamide (MDV3100) purchased from Selleck
Method Western blots/qPCR
Cell Lines CWR-R1 cells
Concentrations 10 μM
Incubation Time 48 h
Results MDV3100 treatment reverses androgen-mediated decreases of Sox2 protein and mRNA in CWR-R1 cells 48 hours after a 24 hour pretreatment with R1881.

Click to enlarge
Source PLoS One 2013 8, e53701. Enzalutamide (MDV3100) purchased from Selleck
Method qPCR
Cell Lines prostate cancer cell lines
Concentrations 10 μM
Incubation Time 30 d
Results There is a significant decrease in PSA expression under continuous AR inhibition with MDV3100.

Product Use Citation (17)

Tech Support & FAQs

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Androgen Receptor Products

  • LCZ696

    LCZ696, consisting of valsartan and sacubitril in 1:1 molar ratio, is an orally bioavailable, dual-acting angiotensin receptor-neprilysin inhibitor (ARNi) for hypertension and heart failure. Phase 3.

  • Endoxifen HCl

    Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.

  • Licochalcone A

    Licochalcone A is an estrogenic flavanoid extracted from licorice root, showing antimalarial, anticancer, antibacterial and antiviral activities. Phase 3.

  • Bicalutamide

    Bicalutamide is an androgen receptor (AR) antagonist with IC50 of 0.16 μM in LNCaP/AR(cs)cell line.

  • ARN-509

    ARN-509 is a selective and competitive androgen receptor inhibitor with IC50 of 16 nM in a cell-free assay, useful for prostate cancer treatment. Phase 3.

  • Dehydroepiandrosterone (DHEA)

    Dehydroepiandrosterone is an important endogenous steroid hormone, which is an androgen receptor antagonist and an estrogen receptor agonist.

  • Galeterone

    Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2.

  • Flutamide

    Flutamide is an antiandrogen drug, with its active metablolite binding at androgen receptor with Ki values of 55 nM, and primarily used to treat prostate cancer.

  • MK-2866 (GTx-024)

    MK-2866 (GTx-024) is a selective androgen receptor modulator (SARM) with Ki of 3.8 nM, and is tissue-selective for anabolic organs. Phase 3.

    Features:The most potent and tissue-selective in vivo activity of SARMs to date, with favorable pharmacokinetic properties.

  • Cyproterone Acetate

    Cyproterone acetate is an androgen receptor (AR) antagonist with IC50 of 7.1 nM, as well as a weak progesterone receptor agonist with weak pro-gestational and glucocorticoid activity.

Recently Viewed Items

Tags: buy Enzalutamide (MDV3100) | Enzalutamide (MDV3100) ic50 | Enzalutamide (MDV3100) price | Enzalutamide (MDV3100) cost | Enzalutamide (MDV3100) solubility dmso | Enzalutamide (MDV3100) purchase | Enzalutamide (MDV3100) manufacturer | Enzalutamide (MDV3100) research buy | Enzalutamide (MDV3100) order | Enzalutamide (MDV3100) mouse | Enzalutamide (MDV3100) chemical structure | Enzalutamide (MDV3100) mw | Enzalutamide (MDV3100) molecular weight | Enzalutamide (MDV3100) datasheet | Enzalutamide (MDV3100) supplier | Enzalutamide (MDV3100) in vitro | Enzalutamide (MDV3100) cell line | Enzalutamide (MDV3100) concentration | Enzalutamide (MDV3100) nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us