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.

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Cited by 41 Publications

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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 NV6z[FFTS3m2b4TvfIlkKEG|c3H5 NEHwVlg4KGSjeYO= NHXy[mo6PSViRYTPTC=> M1G0NWlEPTB;NT6xNkDPxE1? MYGyN|cyOzV4Nx?=
human LNCAP NWrzRWJwTnWwY4Tpc44hSXO|YYm= M4mxTFEh|ryP MYjEUXNQ NH\BclhKdmirYnn0d{Bxem:|dHH0[UB{eGWlaX\pZ{BidnSrZ3XuJJNm[3KndHnvckBqdiCqdX3hckBNVkODUDDj[YxteyCneIDy[ZN{cW6pIHHu[JJw\2WwIILlZ4VxfG:{IHH0JFExOC1zMECwcm0> MmLGNlAzOTh5MUe=
VCaP MV\GeY5kfGmxbjDBd5NigQ>? M4rLelExKM7:TR?= M2LuRlI1KGh? NXuzWY1tTE2VTx?= MlrjV5VxeHKnc4Pld{BtcWejbnStcYVlcWG2ZXSgRXIuTkxic3nncoFtcW6pIB?= MW[yNlcyODR|Nh?=
BCK4 NEj3NXhHfW6ldHnvckBCe3OjeR?= NUnxSnB5OTBizszN M4jk[lch\GG7cx?= NXfFZWVoTE2VTx?= MnjRTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? NHjm[2gzPDR3MUGwPS=>
MCF7s Mny0SpVv[3Srb36gRZN{[Xl? NE\KVG4yOCEQvF2= MUC2JIRigXN? MmrHSG1UVw>? MULJcohq[mm2czDld5Rz[WSrb3ytcYVlcWG2ZXSgdJJwdGmoZYLheIlwdg>? NEi0WZczPDR3MUGwPS=>
PC-3 M{DWd2Z2dmO2aX;uJGF{e2G7 NXHnR29yOTBizszN Mnr3O|IhcA>? NUKxc2dkTE2VTx?= NH3PPFZFd2W|IH7veEBqdmirYnn0JINmdGxicILvcIln\XKjdHnvci=> NXzyRWhGOjV|NES4OlQ>
CWR22Rv1 NV74TJhYTnWwY4Tpc44hSXO|YYm= M1ziTlE2KM7:TR?= Mn3INlQhcA>? M13JfmROW09? NYHHe4FRTG:nczDuc5Qh[W[oZXP0JJRp\SCodXzsJIxmdme2aDDBVkBmgHC{ZYPzbY9v NVrSfZFvOjN5MUO1Olc>

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7; 

PubMed: 28607007     


Treatment of VCaP cells with NOTCH inhibitor, GSI-1, in combination with Enzalutamide (Enz) augmentes its effects on the inhibition of AR, ERG, PSA, NOTCH1 and NOTCH2 expression and induces cleavage of PARP1 and Caspase 7

AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166); 

PubMed: 26378044     


LNCaP95 (LN95) cells were maintained in medium containing 5% CSS and then treated with 5μM of enzalutamide (ENZ) for 0-24 hours. Whole cell lyses were extracted. AR-FL, AR-v7, phosphor-AR(ser213), phosphorAkt(ser473), total Akt, total PP-1, phosphor-Mdm2(ser166), total Mdm2 and β-actin were measured by immunoblotting.

CXCR7; 

PubMed: 29277895     


Western blotting is used to analyze CXCR7 protein levels in VCaP and C4-2B cells.

28607007 26378044 29277895
Growth inhibition assay
Cell proliferation; 

PubMed: 28115200     


Proliferation of the LNCaP prostate cancer cell line, the Ramos Burkitt's cell line, and the Granta, Jeko-1, Rec-1 and Maver-1 MCL cell lines plated in charcoal stripped serum for 96 hours in the absence or presence of enzalutamide (10uM). Data are representative of 3 independent experiments.

28115200
Immunofluorescence
AR; 

PubMed: 27588408     


Representative immunofluorescent images show the expression and subcellular localization of AR in 22Rv1 cells overexpressing PIP5K1α that were treated with vehicle control, enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B.

pAKT(S473); 

PubMed: 27588408     


Representative immunofluorescent images of subcellular localization of pAKT S473 expression in PC3 cells expressing AR-V7 that were treated with vehicle control (Ctrl), enzalutamide, ISA-2011B and combination of enzalutamide and ISA-2011B (ENZ+ISA2011B). The cancer cells are indicated by the arrows.

CXCR7; 

PubMed: 29277895     


Immunofluorescence staining is used to analyze CXCR7 protein levels in prostate cancer cells.

27588408 29277895
ELISA
osteoprotegerin; 

PubMed: 27015557     


MDA-MB-231 cells were treated with 10 μM enzalutamide or vehicle for 48 hours. Levels of OPG (osteoprotegerin) in the supernatant of MDA-MB-231 cells as determined by ELISA. Data are representative of 2 independent experiments.

27015557
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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
5% DMSO+1% CMC Na+1% Tween-80
For best results, use promptly after mixing.
17mg/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.

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
NCT03834493 Not yet recruiting Prostatic Neoplasms Merck Sharp & Dohme Corp. July 15 2019 Phase 3
NCT03834493 Not yet recruiting Prostatic Neoplasms Merck Sharp & Dohme Corp. July 15 2019 Phase 3
NCT03850795 Not yet recruiting Prostate Cancer Metastatic|Castration-resistant Prostate Cancer Hinova Pharmaceuticals USA Inc. May 2019 Phase 3
NCT03834519 Not yet recruiting Prostatic Neoplasms Merck Sharp & Dohme Corp. May 15 2019 Phase 3
NCT03850795 Not yet recruiting Prostate Cancer Metastatic|Castration-resistant Prostate Cancer Hinova Pharmaceuticals USA Inc. May 2019 Phase 3
NCT03834519 Not yet recruiting Prostatic Neoplasms Merck Sharp & Dohme Corp. May 15 2019 Phase 3

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Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

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Frequently Asked Questions

  • Question 1:

    I would like to inquire about the usage or solubility of S1250, Enzalutamide.

  • Answer:

    For in vivo experiment, S1250 can be dissolved in 2% DMSO+30% PEG 300+ddH2O at 5mg/ml as a suspension for oral gavage. And it can be dissolved in 15% DMSO+85% PEG 300 at 10mg/ml as a clear solution. When prepare the solution, please dissolve the compound in DMSO clearly first, then add PEG.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID