Enzalutamide (MDV3100) 化学構造
分子量: 464.44



Quality Control & MSDS


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情報 Enzalutamide (MDV3100)は、36nMのIC50をもつアンドロゲン受容体(AR)敵対者です。
目標 Androgen-receptor
IC50 36 nM [1]
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]
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]
臨床試験 Enzalutamide is currently in Phase III clinical trial in progressive metastatic prostate cancer.

推薦された実験操作 (公開の文献だけ)

キナーゼアッセイ: [3]

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]

細胞系 LNCaP or LNCaP/AR cells
濃度 0-10 μM
処理時間 1-4 days
方法 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.

動物実験: [1]

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
管理 Administered via gavage daily



Download Enzalutamide (MDV3100) SDF
分子量 464.44


CAS No. 915087-33-1
別名 N/A
溶解度 (25°C)
  • DMSO 93 mg/mL
  • 水 <1 mg/mL
  • エタノール <1 mg/mL
保管 2年 -20°C
6月-80°Cin DMSO


カスタマーレビュー (2)

Click to enlarge
Source PLoS One, 2013, 8(1), e53701. Enzalutamide (MDV3100) purchased from Selleck
Method Western blots/qPCR
Cell Lines CWR-R1 cells
Concentrations 10 μM
Incubation Time 48 h
Results MDV3100 treatment reverses androgen-mediated decreases of Sox2 protein and mRNA in CWR-R1 cells 48 hours after a 24 hour pretreatment with R1881.

Click to enlarge
Source PLoS One, 2013, 8(1), e53701. Enzalutamide (MDV3100) purchased from Selleck
Method qPCR
Cell Lines prostate cancer cell lines
Concentrations 10 μM
Incubation Time 30 d
Results There is a significant decrease in PSA expression under continuous AR inhibition with MDV3100.

製品表彰状 (8)

  • Distinct expression and activity of GSK-3α and GSK-3β in prostate cancer. [Darrington RS, et al. Int J Cancer 2012;131(6):E872-83]

    PubMed: 22539113
  • ASC-J9 suppresses castration-resistant prostate cancer growth through degradation of full-length and splice variant androgen receptors. [Yamashita S, et al. Neoplasia 2012;14(1):74-83]

    PubMed: 22355276
  • Structural and functional association of androgen receptor with telomeres in prostate cancer cells. [Zhou J, et al. Aging 2013;5(1):3-17]

    PubMed: 23363843
  • New Therapeutic Approach to Suppress Castration-Resistant Prostate Cancer Using ASC-J9 via Targeting Androgen Receptor in Selective Prostate Cells. [Lai KP, et al. Am J Pathol 2013;182(2):460-73]

    PubMed: 23219429
  • FoxA1 corrupts the antiandrogenic effect of bicalutamide but only weakly attenuates the effect of MDV3100 (Enzalutamide™). [Belikov S, et al. Mol Cell Endocrinol 2013;365(1):95-107]

    PubMed: 23063623
  • Growth kinetics of CD133-positive prostate cancer cells. [Reyes EE, et al. Prostate 2012;73(7):724-33]

    PubMed: 23138940
  • Constitutively active androgen receptor variants upregulate expression of mesenchymal markers in prostate cancer cells. [Cottard F, et al. PLoS One 2013;8(5):e63466]

    PubMed: 23658830
  • Sox2 is an androgen receptor-repressed gene that promotes castration-resistant prostate cancer. [Kregel S, et al. PLoS One 2012;8(1):e53701]

    PubMed: 23326489



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