Enzalutamide (MDV3100)

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

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Enzalutamide (MDV3100) Chemical Structure

Enzalutamide (MDV3100) Chemical Structure
Molecular Weight: 464.44

Validation & Quality Control

Customer Reviews(2)

Quality Control & MSDS

Related Compound Libraries

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

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Product Information

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  • Research Area

Product Description

Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Targets Androgen-receptor
IC50 36 nM [1]
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]
In vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]
Features

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
Dosages 10 mg/kg
Administration Administered via gavage daily
Solubility 0.5% CMC/0.25% Tween 80, 30 mg/mL
1

References

Clinical Trial Information( data from http://clinicaltrials.gov)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02012296 Recruiting Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer University of Chicago|National Cancer Institute (NCI) 2013-12 Phase 1|Phase 2
NCT01949337 Not yet recruiting Adenocarcinoma of the Prostate|Hormone-resistant Prostate Cancer|Recurrent Prostate Cancer|Stage IV Prostate Cancer Alliance for Clinical Trials in Oncology|National Cancer Institute (NCI) 2013-12 Phase 3
NCT02003924 Recruiting Nonmetastatic Castration-Resistant Prostate Cancer Medivation, Inc.|Astellas Pharma Inc 2013-12 Phase 3
NCT01990196 Not yet recruiting Prostate Cancer University of California, Los Angeles 2013-12 Phase 2
NCT02008058 Not yet recruiting Metastatic Castrate-Resistant Prostate Cancer UNC Lineberger Comprehensive Cancer Center|Department of Defense|Memorial Sloan-Kettering Cancer Center|Johns Hopkins University|University of Washington|Oregon Health and Science University 2013-12

Chemical Information

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

C21H16F4N4O2S

CAS No. 915087-33-1
Storage 3 years -20℃Powder
6 months-80℃in DMSO
Syonnyms N/A
Solubility (25°C) * In vitro DMSO 93 mg/mL (200 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 0.5% CMC/0.25% Tween 80, 30 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

Preparing Stock Solutions

Stock Solution (1ml DMSO) 1mM 10mM 20mM 30mM
Mass(mg) 0.46444 4.6444 9.2888 13.9332

Research Area

Customer Reviews (2)


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Rating
Source PLoS One, 2013, 8(1), 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
Rating
Source PLoS One, 2013, 8(1), 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 Citations (8)

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