Enzalutamide (MDV3100)



Androgen Receptor阻害剤の選択性比較


製品説明 Enzalutamide (MDV3100)は、36nMのIC50をもつアンドロゲン受容体(AR)敵対者です。
Androgen Receptor [1]
(LNCaP cells)
36 nM
In vitro試験

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 MVPDfZRwfG:6aXOgRZN{[Xl? MlTkO{Bl[Xm| MVu5OUUhTXSRSB?= NFvoZotKSzVyPUWuNVIh|ryP NISz[FYzOzdzM{W2Oy=>
human LNCAP NWHyNodSTnWwY4Tpc44hSXO|YYm= M{TsUFEh|ryP MmD6SG1UVw>? Mni2TY5pcWKrdIOgdJJwe3SjdHWgd5Bm[2moaXOgZY51cWenbjDz[YNz\XSrb36gbY4hcHWvYX6gUG5ESVBiY3XscJMh\XiycnXzd4lv\yCjbnTyc4dmdiC{ZXPldJRweiCjdDCxNFAuOTByMH7N M4XXS|IxOjF6N{G3
VCaP NFXqXHNHfW6ldHnvckBCe3OjeR?= NGrLWXkyOCEQvF2= Ml;wNlQhcA>? NHTyPYhFVVOR NVqzbGlHW3WycILld5NmeyCuaXfhcoQudWWmaXH0[YQhSVJvRlygd4lodmGuaX7nJC=> M4LGRVIzPzFyNEO2
BCK4 MYHGeY5kfGmxbjDBd5NigQ>? MoXXNVAh|ryP MX63JIRigXN? NGPrZY1FVVOR MljvTY5pcWKrdIOg[ZN1emGmaX;sMY1m\GmjdHXkJJBzd2yrZnXyZZRqd25? MX:yOFQ2OTFyOR?=
MCF7s MkDCSpVv[3Srb36gRZN{[Xl? MlG1NVAh|ryP NVzVboNVPiCmYYnz Mkj1SG1UVw>? M1i1[GlvcGmkaYTzJIV{fHKjZHnvcE1u\WSrYYTl[EBxem:uaX\ldoF1cW:w MlHONlQ1PTFzMEm=
PC-3 NU\o[XJ3TnWwY4Tpc44hSXO|YYm= MljzNVAh|ryP MXG3NkBp NE[1RoxFVVOR MkWxSI9meyCwb4SgbY5pcWKrdDDj[YxtKHC{b3zp[oVz[XSrb36= Ml\0NlU{PDR6NkS=
CWR22Rv1 MXnGeY5kfGmxbjDBd5NigQ>? MYSxOUDPxE1? MmHDNlQhcA>? MYDEUXNQ MVjEc4V{KG6xdDDh[oZm[3RidHjlJIZ2dGxibHXu[5RpKEGUIHX4dJJme3Orb36= MWWyN|cyOzV4Nx?=

... Click to View More Cell Line Experimental Data

In vivo試験 Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]


+ 展開

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.
細胞アッセイ: [1]
+ 展開
  • 細胞株: LNCaP or LNCaP/AR cells
  • 濃度: 0-10 μM
  • 反応時間: 1-4 days
  • 実験の流れ: 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.
+ 展開
  • 動物モデル: Castration-resistant LNCaP/HR xenografts in male SCID mice
  • 製剤: Formulated in 1% carboxymethyl cellulose, 0.1% Tween-80, 5% DMSO
  • 投薬量: 10 mg/kg
  • 投与方法: Administered via gavage daily

溶解度 (25°C)

体外 DMSO 92 mg/mL (198.08 mM) warming
Water <1 mg/mL
Ethanol <1 mg/mL
体内 15% DMSO+85% PEG 300 10mg/mL

* <1 mg/mlは製品が微弱に溶解する或いは溶解しないことを示します。
* 溶解度検測はSelleck技術部門によって行いますので、文献より提供された溶解度と差異がある可能性がありますが、生産工芸と不同ロット(lot)で起きる正常な現象ですから、ご安心ください。


分子量 464.44


CAS No. 915087-33-1
in solvent
別名 N/A





マス (g) = 濃度 (mol/L) x ボリューム (L) x 分子量 (g/mol)


  • マス




貯蔵液を準備することを要求される希釈剤を計算してください. セレック希釈計算器は、以下の方程式に基づきます:

開始濃度 x 開始体積 = 最終濃度 x 最終体積


この方程式は、一般に略語を使われます:C1V1 = C2V2 ( 輸入 輸出 )

  • C1



  • 連続希釈剤

  • 計算結果

  • C1=C0/X C1: LOG(C1):
    C2=C1/X C2: LOG(C2):
    C3=C2/X C3: LOG(C3):
    C4=C3/X C4: LOG(C4):
    C5=C4/X C5: LOG(C5):
    C6=C5/X C6: LOG(C6):
    C7=C6/X C7: LOG(C7):
    C8=C7/X C8: LOG(C8):




チップス: 化学式は大文字と小文字の区別ができます。C10H16N2O2 c10h16n2o2


マス 濃度 ボリューム 分子量


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



Handling Instructions


  • * 必須


  • 問題1:

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

  • 回答:

    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.

Androgen Receptor信号経路図

Androgen Receptor Inhibitors with Unique Features

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID