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(3)

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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Product Description

Biological Activity

Description Enzalutamide (MDV3100) is an androgen-receptor (AR) antagonist with IC50 of 36 nM.
Targets Androgen Receptor [1]
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]
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
Formulation Formulated in 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO
Dosages 10 mg/kg
Administration Administered via gavage daily
Solubility 0.5% CMC/0.25% Tween 80, 30 mg/mL
* 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.

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

SpeciesBaboonDogMonkeyRabbitGuinea pigRatHamsterMouse
Weight (kg)121031.80.40.150.080.02
Body Surface Area (m2)0.60.50.240.150.050.0250.020.007
Km factor202012128653
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

References

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

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

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2014-10-16)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02194842 Not yet recruiting Prostate Cancer European Organisation for Research and Treatment of Cance  ...more European Organisation for Research and Treatment of Cancer - EORTC|Bayer|Astellas Pharma Europe Ltd. December 2014 Phase 3
NCT02256111 Not yet recruiting Non-metastatic, Hormone naïve Prostate Cancer Duke University November 2014 Phase 2
NCT02215096 Not yet recruiting Cancer GlaxoSmithKline October 2014 Phase 1
NCT02254785 Not yet recruiting Metastatic Castration-Resistant Prostatic Cancer British Columbia Cancer Agency|Sanofi|Ozmosis Research Inc. October 2014 Phase 2
NCT02124668 Not yet recruiting Prostate Cancer|Castration-Resistant Prostate Cancer Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pha  ...more Astellas Pharma Europe B.V.|Medivation, Inc.|Astellas Pharma Inc September 2014 Phase 2

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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
Synonyms
Solubility (25°C) * In vitro DMSO 92 mg/mL (198 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.

Research Area

Customer Reviews (3)


Click to enlarge
Rating
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
Rating
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.

Click to enlarge
Rating
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
Concentrations
Incubation Time 48 h
Results When bicalutamide and MDV3100 were used to block AR, BMP-6 no longer increased the probasin promoter activity in Tramp-C1 and PTENCaP8 when RAW 264.7 cells were present.

Product Citations (13)

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