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Enzalutamide

(Synonyms: MDV3100)
236 Cited Publications
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Based on 236 publication(s) in Google Scholar

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

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  • Pureté : 99.97%
  • CAS No.: 915087-33-1
  • Formule: C21H16F4N4O2S
  • Masse moléculaire:464.44
  • Stockage:
    Powder   -20°C, 3 years , 4°C, 2 years ; In solvent   -80°C, 2 years , -20°C, 1 year
  • Enzalutamide Chemical Structure
    Enzalutamide Chemical Structure
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
  • Experimental Validation Results for Enzalutamide
CAS No.: 915087-33-1
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  • Enzalutamide Chemical Structure
    Enzalutamide Chemical Structure
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    Enzalutamide purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 22;186(13):2748-2764.e22. [Abstract]

    Customer Validation
     Viability analysis of LnAR cells harboring vector or MBOAT2 overexpression. Cells were pretreated with DMSO (ctrl) or 5 μM ENZ (Enzalutamide) for 48 h, followed by 1 μM RSL3 for 24 h.

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Cell. 2023 Jun 22;186(13):2748-2764.e22. [Abstract]

    Customer Validation
     Western blot showing expression of endogenous and ectopic MBOAT2 in LnAR cells harboring either vector control or MBOAT2-mCherry. Cells were treated with 5 μM ENZ (Enzalutamide) as indicated for 48 h.

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: J Endocrinol. 2019 Jan;240(1):51-63. [Abstract]

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

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Eur J Med Chem. 2018 Sep 5:157:1164-1173. [Abstract]

    Customer Validation
     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.

  • 1/16

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

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

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Oct 10;8(1):15063. [Abstract]

    Customer Validation
     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.

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. [Abstract]

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

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Sci Rep. 2018 Nov 23;8(1):17307. [Abstract]

    Customer Validation
     Protein expression analysis of p-STAT3S727, STAT3, PSA, AR and Vinculin in the treatment of ENZ and GPA500.

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Front Physiol. 2018 Apr 16:9:312. [Abstract]

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     C4-2R cells are treated with MK 733, Enzalutamide or combination of the two drugs at the indicated concentrations for 48 hours, followed by Immunoblotting (IB) against cleaved PARP.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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).

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: Prostate. 2017 Feb;77(3):309-320. [Abstract]

    Customer Validation
     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.

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: University of British Columbia. 2017 Apr.

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     The levels of YAP1 protein are measured in LNCaP cells treated for 24 h with the AR antagonist MDV3100 (Enzalutamide, 100 nM) and ICI 176334 (10 mM).

  • 1/16

    Enzalutamide purchased from MedChemExpress. Usage Cited in: University of British Columbia. 2017 Dec.

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

  • 1/16

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

    Customer Validation
     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.

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

    Customer Validation
     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.

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

    Customer Validation
     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.

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

    Customer Validation
     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.

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