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.

Size Price Stock Quantity  
In DMSO USD 300 In stock
USD 150 In stock
USD 270 In stock
USD 770 In stock

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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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)
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 NYLMe2VWS3m2b4TvfIlkKEG|c3H5 M330dVch\GG7cx?= MX65OUUhTXSRSB?= NGjOZ|RKSzVyPUWuNVIh|ryP M2XvZlI{PzF|NU[3
human LNCAP MWPGeY5kfGmxbjDBd5NigQ>? M4jKU|Eh|ryP MnXxSG1UVw>? MWnJcohq[mm2czDwdo9{fGG2ZTDzdIVkcW[rYzDhcpRq\2WwIIPlZ5JmfGmxbjDpckBpfW2jbjDMUmNCWCClZXzsd{BmgHC{ZYPzbY5oKGGwZILv[4VvKHKnY3XweI9zKGG2IEGwNE0yODBybl2= M3jOPFIxOjF6N{G3
VCaP MY\GeY5kfGmxbjDBd5NigQ>? NF3WW4IyOCEQvF2= M4\TblI1KGh? M4i4TWROW09? M4fXbnN2eHC{ZYPz[ZMhdGmpYX7kMY1m\GmjdHXkJGFTNU[OIIPp[45idGmwZzC= M{L6S|IzPzFyNEO2
BCK4 NVLiRppUTnWwY4Tpc44hSXO|YYm= M{P0NlExKM7:TR?= NULFdlJpPyCmYYnz MUPEUXNQ MWnJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? NXmwU4ZFOjR2NUGxNFk>
MCF7s M4fnVWZ2dmO2aX;uJGF{e2G7 MlrmNVAh|ryP MXu2JIRigXN? NYDuW2lkTE2VTx?= NEXpWY5KdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= MmnLNlQ1PTFzMEm=
PC-3 Ml\0SpVv[3Srb36gRZN{[Xl? MoXCNVAh|ryP NF;j[3U4OiCq M1jsZWROW09? M1O2RmRw\XNibn;0JIlvcGmkaYSgZ4VtdCCycn;sbYZmemG2aX;u NGW1NFkzPTN2NEi2OC=>
CWR22Rv1 M4\GSWZ2dmO2aX;uJGF{e2G7 MW[xOUDPxE1? NID5R2UzPCCq MXLEUXNQ NFnKSZRFd2W|IH7veEBi\m[nY4SgeIhmKG[3bHygcIVv\3SqIFHSJIV5eHKnc4Ppc44> NVX2fVNKOjN5MUO1Olc>

... 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

Kinase Assay
+ 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
+ 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
+ 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 (198.08 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+30% PEG 300+ddH2O 5mg/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 Information

Molecular Weight 464.44
Formula

C21H16F4N4O2S

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
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|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 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
NCT02339168 Recruiting Prostate Cancer University of California, Davis|National Cancer Institute (NCI)|Medivation, Inc.|Astellas Pharma Inc June 2016 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID