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Enzalutamide (Synonyms: MDV3100)

Cat. No.: HY-70002 Purity: 99.71%
Handling Instructions

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

For research use only. We do not sell to patients.

Enzalutamide Chemical Structure

Enzalutamide Chemical Structure

CAS No. : 915087-33-1

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Customer Review

Other Forms of Enzalutamide:

Customer Validation

    Enzalutamide purchased from MCE. Usage Cited in: Mol Cancer Ther. 2013 May;12(5):567-76.

    LNCaP cells are treated with Compound 30 or MDV3100 for 24 hours; AR and PSA are analyzed by Western blot analysis; Vinculin is used as a loading control.

    Enzalutamide purchased from MCE. Usage Cited in: Cancer Res. 2013 Aug 15;73(16):5206-17.

    CLU is induced by MDV3100 in time- and dose-dependent manner. LNCaP cells are treated with MDV3100 at indicated time (left) or concentration (right) and Western blot analysis is conducted with CLU, AR, and PSA antibodies.

    Enzalutamide purchased from MCE. Usage Cited in: Cancer Res. 2013 Aug 15;73(16):5206-17.

    MDV3100-induced CLU is mediated via p90Rsk-YB-1 signaling pathway. MDV3100 activates AKT and MAPK pathways. LNCaP cells are treated with 10 μM MDV3100 for indicated times and Western blotted using CLU, p-Rsk/R/Rsk, p-S6K/S6K, and pYB-1/YB-1. Vinculin is used as a loading control.

    Enzalutamide purchased from MCE. Usage Cited in: Mol Cancer Res. 2016 Jun;14(6):574-85.

    LNCaP and DuCaP cells are 1 treated for 72 hours with 1 or 10 μM Enzalutamide in the presence of increasing IL6 concentrations. The effect on JAK/STAT3 signaling is measured by determining STAT3 Tyr705-phosphorylation via Western blot and calculation of dose response curves.

    Enzalutamide purchased from MCE. Usage Cited in: Mol Cancer Ther. 2016 Sep;15(9):2107-18.

    Combination of Enzalutamide and 17-AAG lead to decreased AR protein level and transcriptional activity. (A&B) LNCaP (A) and C4-2 (B) cells are treated as indicated for 24 hr, followed by IB against AR, PSA and CHIP. (C&D) 22RV1 (C) and MR49F (D) cells are treated as indicated for 24 hr, followed by IB against AR and HSP90. (E) C4-2 cells are treated as indicated for 24 hr, fractionated into cytoplasm and nuclear, followed by IB against AR and Plk1.

    Enzalutamide purchased from MCE. Usage Cited in: Prostate. 2017 Feb;77(3):309-320.

    LNCaP cell are treated with 20 mM LY294002 or 10 mM U0126 for 1 hr before 10 mM of ENZ. Whole-cell extracts are subjected to SDS–PAGE, followed by western blot analysis for the indicated proteins.

    Enzalutamide purchased from MCE. Usage Cited in: Int J Oncol. 2017 Jan;50(1):75-84.

    Effects of culture in CSS and treatment with Enzalutamide on cell cycle of T24GR cells. T24 and T24GR cells (5x105) are seeded in a 6-well plate and cultured for 24 h. The culture medium is changed to that containing 50 μM Enzalutamide or vehicle (DMSO). Seventy-two hours later, cell lysates are harvested and subjected to western blot analysis for cyclin B1, D1 and β-actin.

    Enzalutamide purchased from MCE. Usage Cited in: Patent. US20140088178A1.

    Effect of AR1 (MDV-3100) administration on AKT and ERK phosphorylation and protein levels in LNCaP cells. (A), 10 μM AR1. (B), after 48 hours of AR1 treatment at indicated concentrations. (C), Dose dependent change of expression level of AKT or ERK after treatment with AR1. (D), Dose dependent change of expression level of AKT or ERK after treatment with AR1.

    Enzalutamide purchased from MCE. Usage Cited in: Oncotarget. 2016 Jun 28;7(26):40690-40703.

    Dihydrotestosterone (DHT) alone, Enzalutamide alone, or the combination in androgen-depleted conditions also increase expression of canonical AR targets: KLK3, TMPRSS2, and NKX3.1 and increase protein levels of PSA encoded by the KLK3 gene.

    Enzalutamide purchased from MCE. Usage Cited in: Cancer Discov. 2017 Jan;7(1):54-71.

    BRN2 expression inversely correlates with PSA in human PCa and is induced by ENZ. Protein and relative mRNA expression of BRN2, SYP, NSE, CGA, and VINC in siScr and 796 siBRN2 16DCRPC cells treated -/+ 10 μM ENZ for 2, 4 or 7 days.

    Enzalutamide purchased from MCE. Usage Cited in: Oncotarget. 2016 Sep 13;7(37):59781-59794.

    Short term treatment (14 days) of LAPC4 vehicle cells with 8μM Enzalutamide clearly demonstrates that AR overexpression is not a short term effect of drug treatment but develops as a long term adaptation during acquisition of resistance. It has been suggested that presence of a truncated AR variant (AR-V7) is associated with resistance to Enzalutamide.

    Enzalutamide purchased from MCE. Usage Cited in: Department of Medicine, Faculty of Obstetrics and Gynaecology. University of British Columbia. Apr 18, 2017.

    VCaP (mock) and VCaP (UGT2B17) cells are cultured in the RPMI1640 medium plus 5% CSS. Cells are treated with vehicle, 10 nM of R1881 or 10 μM of Enzalutamide (ENZ) for 0 or 28 days. Protein levels of UGT2B17, pSrc, tSrc, pAKT, total AKT, pSTAT3, total STAT3, pSTAT5, total STAT5 and β-actin are determined by immunoblotting.

    Enzalutamide purchased from MCE. Usage Cited in: Horm Cancer. 2017 Aug;8(4):243-256.

    LNCaP cells are grown in complete media for 24 h in the presence of vehicle (control) or Enzalutamide, 10 μM, and protein expression normalized to β-tubulin.

    Enzalutamide purchased from MCE. Usage Cited in: Oncotarget. 2015 Aug 21;6(24):20474-84.

    LNCaP cells are cultured in RPMI1640 medium containing 5% CSS and treated with vehicle, 1 μM of ICRF187 or 1 μM of ICRF193 in addition to vehicle, 10 nM of R1881 or 10 μM of ENZ treatment for 2 hours. Three independent ChIP experiments are performed using the AR antibody. AR protein levels under 2 and 24 hour treatment are detected by Western blotting.

    Enzalutamide purchased from MCE. Usage Cited in: Mol Cancer Ther. 2017 Oct;16(10):2281-2291.

    Top-Cells (RPMI+CSS) are co-transfected with ARR3tk-Luc and Renilla-Luc plasmids (48 hrs). With the exception of 22Rv1, 0.1 nM R1881 is used to stimulate the AR, followed by compound treatment (24 hrs). 100% refers to normalized luminescence without compound (DMSO vehicle). Curves are fitted to a sigmoid dose-response with variable slope equation (GraphPad).

    Enzalutamide purchased from MCE. Usage Cited in: Oncotarget. 2017 Dec 7;8(70):115054-115067.

    The levels of YAP1 protein are measured in LNCaP cells treated for 24 h with the AR antagonist MDV3100 (Enzalutamide, 100 nM) and Casodex (Bicalutamide, 10mM).

    Enzalutamide purchased from MCE. Usage Cited in: Front Physiol. 2018 Apr 16;9:312.

    Protein lysates of vehicle-, 1 μM BCT-, and 1 μM EZT-treated MDA-MB-453 cells are probed by immunoblotting with anti-KCa1.1 (upper panel) and anti-ACTB (lower panel) antibodies on the same filter.

    Enzalutamide purchased from MCE. Usage Cited in: Faculty of Medicine. University of British Columbia. December 2017.

    p-TNIK (S764), T-TNIK, and PSA protein expression are assessed in (A) LNCaP and 16DCRPC cells that are treated with 10 μM Enzalutamide (ENZ) in media containing 10% FBS for 2, 4, and 7 days by western blot. Vinculin is used as loading control.

    Enzalutamide purchased from MCE. Usage Cited in: Mol Cancer Ther. 2013 May;12(5):567-76.

    LNCaP cells are maintained in androgen-deprived conditions for 24 hours and treated with 10 μM Compound 30 or MDV3100 for 2 hours followed by addition of 1 nM of R1881. After 15 minutes incubation, cells are fixed and AR localization is assessed by immunofluorescence imaging.

    Enzalutamide purchased from MCE. Usage Cited in: Sci Rep. 2016 Sep 28;6:33968.

    Representative images of 22Rv1 cells transduced with PSEBC-TSTA and showing that single cell luminescence increases with exposure time but not the number of detected cells. Bioluminescence microscopy can titrate AR agonist DHT (0.5-10 nM) concentration ability to activate AR-transcription. LAPC4-GFP cells are infected with PSEBC-TSTA in media containing 0.5 to 10 nM of Dihydrotestosterone (DHT).

    Enzalutamide purchased from MCE. Usage Cited in: Sci Rep. 2017 Jun 8;7(1):3058.

    CXCR7 mRNA in cells treated with 2 µM Bicalutamide (BiC) relative to untreated (UT) cells.

    Enzalutamide purchased from MCE. Usage Cited in: Prostate. 2018 Sep 3.

    Treatment with sub-dose of Everolimus (10 nM), together with CQ (5 µM) increases the levels of Bax and cleaved PARP, and decreases the levels of Bcl-2 expression in both PC3 and LNPER cells.

    Enzalutamide purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656.

    Evaluation of protein expression change of Notch receptors response to the treatment of 10 μM Enzalutamide as an androgen receptor (AR) antagonist.

    Enzalutamide purchased from MCE. Usage Cited in: Int J Cancer. 2018 Aug 1;143(3):645-656.

    Evaluation of expression change of Notch downstream under the androgen-deprived condition with or without the treatment of DAPT by western blot assay.

    Enzalutamide purchased from MCE. Usage Cited in: J Biol Chem. 2018 Sep 14;293(37):14328-14341.

    C4-2R cells are treated with Simvastatin, Enzalutamide or combination of the two drugs at the indicated concentrations for 48 hours, followed by Immunoblotting (IB) against cleaved PARP.

    Enzalutamide purchased from MCE. Usage Cited in: Eur J Med Chem. 2018 Sep 5;157:1164-1173.

    Dose-response curves of active degraders and Enzalutamide on AR transcriptional activity as measured in LNCaP-eGFP cells following 0.1 nM R1881 for 72 hours in RPMI+CSS media (3 replicates per point). (B) PSA inhibition curves against transcriptional activity of AR as measured from the media of LNCaP-eGFP cells with active degraders and enzalutamide under the same conditions as A.

    Enzalutamide purchased from MCE. Usage Cited in: Sci Rep. 2018 Oct 10;8(1):15063.

    The increased protein levels of both LEDGF/p75 and CLU are observed in cells treated with either 1 nM or 10 nM DHT, which is attenuated by exposure to 1 μM Enz.

    Enzalutamide purchased from MCE. Usage Cited in: J Endocrinol. 2018 Oct 1. pii: JOE-18-0503.R1.

    At the protein level, CORT-induced FKBP5 content in both WAT and liver is attenuated with AR antagonism.

    Enzalutamide purchased from MCE. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. 

    Western analysis of protein expression in LNCaP and 16D CRPC cells treated with 10 μM ENZ for indicated days.

    Enzalutamide purchased from MCE. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. 

    Protein expression analysis of p-STAT3S727, STAT3, PSA, AR and Vinculin in the treatment of ENZ and GPA500.
    • Biological Activity

    • Protocol

    • Technical Information

    • Purity & Documentation

    • References

    Description

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

    IC50 & Target

    IC50: 36 nM (androgen-receptor, in LNCaP cells)[1]

    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 inhibits 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]. Enzalutamide shows dose-independent pharmacokinetics at intravenous and oral doses of 0.5-5 mg/kg[4].

    Clinical Trial
    Solvent & Solubility
    In Vitro: 

    DMSO : ≥ 50 mg/mL (107.66 mM)

    H2O : < 0.1 mg/mL (insoluble)

    *"≥" means soluble, but saturation unknown.

    Preparing
    Stock Solutions
    Concentration Solvent Mass 1 mg 5 mg 10 mg
    1 mM 2.1531 mL 10.7657 mL 21.5313 mL
    5 mM 0.4306 mL 2.1531 mL 4.3063 mL
    10 mM 0.2153 mL 1.0766 mL 2.1531 mL
    *Please refer to the solubility information to select the appropriate solvent.
    In Vivo:
    • 1.

      Add each solvent one by one:  10% DMSO    90% corn oil

      Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    • 2.

      Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

      Solubility: ≥ 2.5 mg/mL (5.38 mM); Clear solution

    References
    Cell Assay
    [1]

    LNCaP cells (107 cells/condition) are grown in RPMI media supplemented with 5% charcoalstripped serum for 22 days, then treated with DMSO or 1 nM R1881, combined with an antiandrogen (DMSO, 1 μM Bicalutamide, 10 μM Bicalutamide, 1 μM RD162, 10 μM RD162, 1 μM MDV3100, or 10 μM MDV3100) for 8 hours. An aliquot of cells are harvested for qRT-PCR of PSA and TMPRSS2 mRNA. The remaining cells are cross-linked using 1% paraformaldehyde for 10 minutes, then glycine is added and samples centrifuged (4°C, 4000 rpm, 5 minutes) to stop further crosslinking. Chromatin immunoprecipitation is performed using a chromatin immunoprecipitation assay kit. Immunoprecipitated DNA is amplified by real-time PCR. Primers are PSA enhancer forward-ATGTTCACATTAGTACACCTTGCC and reverse-TCTCAGATCCAGGCTTGCTTACTGTC and TMPRSS2 enhancer forward-TGGTCCTGGATGATAAAAAAAGTTT and reverse-GACATACGCCCCACAACAGA[1].

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    Animal Administration
    [3][4]

    Mice[3]
    Following a 5-day acclimation period, 5- to 9-week-old male CB17SCID mice are castrated and allowed to recover for an additional 5 days before inoculation with tumor cells. LNCaP cells co-expressing exogenous AR and the AR-dependent reporter construct ARR2-Pb-Luc (LNCaP-AR-Lux cells) are used to generate a xenograft model of human prostate cancer. Before implantation, LNCaP-AR-Lux cells are prepared by the addition of trypsin-EDTA, washed with complete medium, collected and resuspended at 20×106 cells/mL. Cell suspensions are diluted with Matrigel to 2×106 cells/0.2 mL and delivered subcutaneously in the suprascapular region. Tumor growth is monitored to the volume of 100 mm3 when treatment begins (80 days). The observed rate of tumor take with LNCaP-AR-Lux cells is between 70% and 80%. Body weight and tumor volumes (width2×length/2) are measured two to three times per week with a digital caliper, and the average tumor volumes are determined. Test drugs are diluted in Tween 80:PEG 400, and stored at 4°C until administration by oral gavage. Each group of mice (n=7) is treated daily for 28 consecutive days with 1, 10, or 50 mg/kg Enzalutamide, vehicle control, or 50 mg/kg Bicalutamide. At the end of the treatment period or when tumor volume exceeded 1,000 mm3, animals are euthanized and blood and tissue samples are collected for analysis.
    Rats[4]
    Male SD rats (n=3) are administered Enzalutamide through the tail vein (intravenous) and by oral gavage at 1 mg/kg and are kept in metabolic cages after dosing. Urine and feces samples are collected over the following time intervals after dosing: 0-2, 2-4, 4-6, 6-10, 10-24, 24-48, and 48-72 h. The metabolic cages are rinsed with distilled water, and residues are added to the urine samples at 72 h. To extract the Enzalutamide present in the feces, samples are shaken vigorously for 12 h with 50 % methanol.

    MCE has not independently confirmed the accuracy of these methods. They are for reference only.

    References
    Molecular Weight

    464.44

    Formula

    C₂₁H₁₆F₄N₄O₂S

    CAS No.

    915087-33-1

    SMILES

    S=C(N(C(C1(C)C)=O)C2=CC=C(C#N)C(C(F)(F)F)=C2)N1C3=CC(F)=C(C(NC)=O)C=C3

    Storage
    Powder -20°C 3 years
      4°C 2 years
    In solvent -80°C 6 months
      -20°C 1 month
    Shipping

    Room temperature in continental US; may vary elsewhere

    Purity: 99.71%

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    Product Name:
    Enzalutamide
    Cat. No.:
    HY-70002
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    Enzalutamide

    Cat. No.: HY-70002