Enzalutamide (MDV3100)

製品コードS1250 バッチS125016

印刷

化学情報

Chemical Structure Synonyms MDV3100 Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C21H16F4N4O2S
分子量 464.44 CAS No. 915087-33-1
Solubility (25°C)* 体外 DMSO 92 mg/mL (198.08 mM)
Ethanol 24 mg/mL (51.67 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 1.500mg/ml (3.23mM) Taking the 1 mL working solution as an example, add 50 μL of 30 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.500mg/ml (5.38mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* 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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 エンザルタミド (Enzalutamide (MDV3100)) は、アンドロゲン受容体 (androgen receptor, AR) アンタゴニストで LNCaP 細胞における IC50 は36 nM です。エンザルミドはオートファジー (autophagy) を増加させることが示されています。
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 this compound shows no agonism in LNCaP/AR prostate cells. It antagonizes induction of prostate-specific antigen (PSA) and transmembrane serine protease 2 (TMPRSS2), combination with the synthetic androgen R1881 in parental LNCaP cells. This chemical could inhibit the transcriptional activity of a mutant AR protein (W741C, mutation of Trp741 to Cys). [1] It 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]

プロトコル(参考用のみ)

キナーゼアッセイ 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 this compound 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 this compound 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 this chemical. After two days of incubation, reporter activities are assayed.
細胞アッセイ 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 this compound in media containing 5-10% charcoal-stripped serum.
動物実験 動物モデル Castration-resistant LNCaP/HR xenografts in male SCID mice
投薬量 10 mg/kg
投与方法 Administered via gavage daily

参考

  • https://pubmed.ncbi.nlm.nih.gov/19359544/
  • https://pubmed.ncbi.nlm.nih.gov/20398925/
  • http://worldwide.espacenet.com/publicationDetails/originalDocument?CC=US&NR=2007254933A1&KC=A1&FT=D&

カスタマーフィードバック

Data from [Cancer Sci, 2013, 104(8), 1027-32]

Data from [PLoS One, 2013, 8, e53701]

Data from [PLoS One, 2013, 8, e53701]

Selleckの高級品が、幾つかの出版された研究調査結果（以下を含む）で使われた：

Circular RMST cooperates with lineage-driving transcription factors to govern neuroendocrine transdifferentiation [ Cancer Cell, 2025, 43(5):891-904.e10] PubMed: 40250444
Targeting histone H2B acetylated enhanceosomes via p300/CBP degradation in prostate cancer [ Nat Genet, 2025, 57(10):2468-2481] PubMed: 41044247
Off-pore nucleoporin sPOM121 transcriptionally propels β-Catenin driven tumor progression and immune escape in prostate cancer [ Cancer Discov, 2025, 10.1158/2159-8290.CD-25-0629] PubMed: 40709833
Engineering bi-directional chemically-modulated synthetic condensates for cellular control [ Nat Commun, 2025, 16(1):6587] PubMed: 40675979
Apolipoprotein E promotes primary resistance to AR-targeted therapy via inducing TRIM25-mediated AR ubiquitination and sensitizes immunotherapy in prostate cancer [ Theranostics, 2025, 15(12):5572-5591] PubMed: 40365288
Clinical Context Shapes the Relationship Between Genomic Alterations and Response to AR Inhibitors and Chemotherapy in Metastatic Prostate Cancer [ Clin Cancer Res, 2025, 10.1158/1078-0432.CCR-24-1812] PubMed: 40227200
Multi-layer stratified oncology platform utilizing transcriptomics, prostate cancer organoids, and modeling of drug response [ J Exp Clin Cancer Res, 2025, 44(1):290] PubMed: 41094672
An Autophagy-Targeting Chimera Induces Degradation of Androgen Receptor Mutants and AR-v7 in Castration-Resistant Prostate Cancer [ Cancer Res, 2025, 85(2):342-359] PubMed: 39531508
PlexinD1 is a driver and a therapeutic target in advanced prostate cancer [ EMBO Mol Med, 2025, 17(2):336-364] PubMed: 39748059
EHMT2-mediated R-loop formation promotes the malignant progression of prostate cancer via activating Aurora B [ Clin Transl Med, 2025, 15(1):e70164] PubMed: 39763034

長期の保管のために-20°Cの下で製品を保ってください。

人間や獣医の診断であるか治療的な使用のためにでない。

各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。