Enzalutamide (MDV3100)

Catalog No.S1250

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

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Enzalutamide (MDV3100) Chemical Structure

Enzalutamide (MDV3100) Chemical Structure
Molecular Weight: 464.44

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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 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 LNCAPNVf4RolPS3m2b4TvfIlkKEG|c3H5MXK3JIRigXN?MljvPVUmKEW2T1i=NUH0XWVNUUN3ME21MlEzKM7:TR?=NHjjVmkzOzdzM{W2Oy=>
human LNCAPMnPvSpVv[3Srb36gRZN{[Xl?MkHrNUDPxE1?NW\rd5pOTE2VTx?=MYLJcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2=NFvnOZYzODJzOEexOy=>
VCaPMofFSpVv[3Srb36gRZN{[Xl?NHnXVJUyOCEQvF2=MnPrNlQhcA>?NEDhNoRFVVORMkXwV5VxeHKnc4Pld{BtcWejbnStcYVlcWG2ZXSgRXIuTkxic3nncoFtcW6pIB?=MmrLNlI4OTB2M{[=
BCK4M3n0NWZ2dmO2aX;uJGF{e2G7NVP2eoU3OTBizszNNV[yR2QyPyCmYYnzMnHaSG1UVw>?MlPqTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25?MVmyOFQ2OTFyOR?=
MCF7sNVn5Noh5TnWwY4Tpc44hSXO|YYm=MnfENVAh|ryPMofMOkBl[Xm|NWPISpprTE2VTx?=NGLDPIxKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?=M2rmRVI1PDVzMUC5
PC-3MUTGeY5kfGmxbjDBd5NigQ>?MkP0NVAh|ryPMVK3NkBpNUnJ[2MxTE2VTx?=MUfEc4V{KG6xdDDpcohq[mm2IHPlcIwheHKxbHnm[ZJifGmxbh?=NVPOeZVsOjV|NES4OlQ>
CWR22Rv1M1jmfmZ2dmO2aX;uJGF{e2G7M4rOT|E2KM7:TR?=MXiyOEBpM2G3V2ROW09?NW\hcolsTG:nczDuc5Qh[W[oZXP0JJRp\SCodXzsJIxmdme2aDDBVkBmgHC{ZYPzbY9vMYCyN|cyOzV4Nx?=

... 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]
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

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

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
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

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 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02711956 Not yet recruiting Metastatic Castration-Resistant Prostate Cancer Zenith Epigenetics October 2016 Phase 1
NCT02684227 Not yet recruiting Endometrial Cancer M.D. Anderson Cancer Center|Astellas Pharma Inc|Medivatio  ...more M.D. Anderson Cancer Center|Astellas Pharma Inc|Medivation, Inc.|National Comprehensive Cancer Network August 2016 Phase 2
NCT02685397 Not yet recruiting Castration-resistant Prostate Cancer Patients With Oligometastases Sir Mortimer B. Davis - Jewish General Hospital August 2016 Phase 2|Phase 3
NCT02833883 Not yet recruiting Prostate Cancer|Castration-resistant Prostate Cancer. Memorial Sloan Kettering Cancer Center|Celgene Corporatio  ...more Memorial Sloan Kettering Cancer Center|Celgene Corporation|Thomas Jefferson University|University of Michigan July 2016 Phase 1
NCT02689427 Not yet recruiting Breast Cancer M.D. Anderson Cancer Center|Astellas Pharma US, Inc. June 2016 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
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 92 mg/mL warming (198.08 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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