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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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 NUPaW25HS3m2b4TvfIlkKEG|c3H5 M{XFO|ch\GG7cx?= M{exR|k2LSCHdF;I M3TVO2lEPTB;NT6xNkDPxE1? MmPoNlM4OTN3Nke=
human LNCAP Mn;ISpVv[3Srb36gRZN{[Xl? NVjI[GlnOSEQvF2= NXTGNmNJTE2VTx?= M1TRXGlvcGmkaYTzJJBzd3O2YYTlJJNx\WOrZnnjJIFvfGmpZX6gd4VkemW2aX;uJIlvKGi3bXHuJGxPS0GSIHPlcIx{KGW6cILld5NqdmdiYX7kdo9o\W5icnXj[ZB1d3JiYYSgNVAxNTFyMEDuUS=> M2nlNFIxOjF6N{G3
VCaP NF\0enBHfW6ldHnvckBCe3OjeR?= MoTVNVAh|ryP NGPwN3kzPCCq MYDEUXNQ NWjWUFlKW3WycILld5NmeyCuaXfhcoQudWWmaXH0[YQhSVJvRlygd4lodmGuaX7nJC=> NIWzPVQzOjdzMESzOi=>
BCK4 NYLDW2NyTnWwY4Tpc44hSXO|YYm= MUGxNEDPxE1? NVTDTG85PyCmYYnz MU\EUXNQ NFLMXIpKdmirYnn0d{Bme3S{YXTpc4wudWWmaXH0[YQheHKxbHnm[ZJifGmxbh?= M1vDUVI1PDVzMUC5
MCF7s M2PZeWZ2dmO2aX;uJGF{e2G7 M3fkclExKM7:TR?= NVrrVplOPiCmYYnz M1\YU2ROW09? NV\hZWJPUW6qaXLpeJMh\XO2cnHkbY9tNW2nZHnheIVlKHC{b3zp[oVz[XSrb36= MWWyOFQ2OTFyOR?=
PC-3 NE\tSllHfW6ldHnvckBCe3OjeR?= Ml[1NVAh|ryP NX\1T|lMPzJiaB?= NHrx[GZFVVOR MmToSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= NYX5S4hbOjV|NES4OlQ>
CWR22Rv1 MYLGeY5kfGmxbjDBd5NigQ>? MYixOUDPxE1? MoDiNlQhcA>? M3nSRmROW09? NEDQWVdFd2W|IH7veEBi\m[nY4SgeIhmKG[3bHygcIVv\3SqIFHSJIV5eHKnc4Ppc44> MmjzNlM4OTN3Nke=

... 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:[3]
+ 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:[1]
+ 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:[1]
+ 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 warmed (198.08 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 15% DMSO+85% PEG 300 10mg/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
NCT01875250 Active, not recruiting Prostate Cancer National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC) May 28, 2013 Phase 2
NCT02403505 Not yet recruiting Stage, Prostate Cancer|Surgery Dr. Han Xu, President/CEO / PD / PI / Monitor / IRB Chair|PPD|Medicine Invention Design, Inc August 2020 Phase 3
NCT02885649 Not yet recruiting Clear Cell Renal Cell Carcinoma|Stage I Renal Cell Cancer Rutgers, The State University of New Jersey|National Cancer Institute (NCI) June 2017 Early Phase 1
NCT02987543 Recruiting Metastatic Castration-resistant Prostate Cancer AstraZeneca February 2017 Phase 3
NCT02953860 Not yet recruiting Breast Cancer University of Colorado, Denver|United States Department of Defense January 2017 Phase 2
NCT02955394 Not yet recruiting Breast Cancer University of Colorado, Denver|United States Department of Defense January 2017 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID