Enzalutamide

別名:MDV3100

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。

Enzalutamide化学構造

CAS No. 915087-33-1

サイズ 価格(税別) 在庫状況
JPY 22500 国内在庫あり
JPY 40500 国内在庫あり
JPY 115500 国内在庫あり
JPY 235500 国内在庫なし(納期7~10日)
JPY 445500 国内在庫あり

代表番号: 045-509-1970|電子メール:[email protected]
よく尋ねられる質問

文献中Selleckの製品使用例(463)

製品安全説明書

現在のバッチを見る: 純度: 99.99%
99.99

Enzalutamideと併用されることが多い化合物

Apalutamide (ARN-509)


Enzalutamide and Apalutamide improve metastasis-free survival (MFS) and overall survival in patients with non-metastatic castration-resistant prostate cancer (M0CRPC).


Swami U, et al. Cancer Treat Res Commun. 2020;25:100205.

Darolutamide (ODM-201)


Enzalutamide and Darolutamide improve metastasis-free survival (MFS) and overall survival in patients with non-metastatic castration-resistant prostate cancer (M0CRPC).


Swami U, et al. Cancer Treat Res Commun. 2020;25:100205.

Bicalutamide


Enzalutamide outperforms Bicalutamide in median progression-free survival (PFS) in patients with metastatic castration-resistant prostate cancer.


Shore ND, et al. Lancet Oncol. 2016;17(2):153-163.

Abiraterone


Enzalutamide and Abiraterone prolong progression-free survival (PFS) and overall survival (OS) in patients with metastatic castration-resistant prostate cancer.


Wang Y, et al. J Cancer Res Clin Oncol. 2018;144(9):1751-1768.

Abiraterone Acetate


Enzalutamide and Abiraterone acetate are second-generation anti-androgens that improve survival in patients with castration-resistant prostate cancer (CRPC).


Moreira-Silva F, et al. Front Oncol. 2022 May 24;12:877379.

Enzalutamide関連製品

Androgen Receptor阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
BCK4 Function Assay 10 μM 7 days Inhibits estradiol-mediated proliferation 24451109
VCaP Function Assay 10 μM 24 h Suppresses ligand-mediated AR-FL signaling 22710436
MCF7s Function Assay 10 μM 6 days Inhibits estradiol-mediated proliferation 24451109
PC-3 Function Assay 10 μM 72 h Does not inhibit cell proliferation 25344864
CWR22Rv1 Function Assay 15 μM 24 h Does not affect the full length AR expression 23713567
human LNCAP Function Assay 1 μM Inhibits prostate specific antigen secretion in human LNCAP cells expressing androgen receptor at 100-1000nM 20218717
human LNCAP Cytotoxic Assay 7 days IC50=5.12 μM 23713567
LNCAP Antagonist activity assay 72 h IC50 = 0.05 μM 30193215
LNCAP Antagonist activity assay 72 h IC50 = 0.09 μM 30193215
LNCAP Antiproliferative activity assay 3 days IC50 = 0.1271 μM 26046313
LNCAP Antagonist activity assay 6 days GI50 = 0.29 μM 28011219
UAS-bla GripTite 293 Antagonist activity assay 16 to 24 h IC50 = 0.361 μM 27301368
mammalian expression system Antagonist activity assay 22 to 24 h EC50 = 0.42 μM 28385503
VCaP Growth inhibition assay 144 h GI50 = 0.61 μM 25121586
LNCaP Antagonist activity assay 2 h EC50 = 0.915 μM 23713567
COS7 Antagonist activity assay 24 h IC50 = 1.26 μM 29117897
AR LBD mutant Antagonist activity assay 4 h IC50 = 1.35 μM 27810589
LNCAP Cytotoxicity assay 7 days GI50 = 5.12 μM 23713567
CWR22Rv1 Cell survival assay 144 h IC50 = 9.7 μM 25121586
LNCAP Antiproliferative activity assay 96 h IC50 = 11.47 μM 27301368
LNCaP-hr Antiproliferative activity assay 3 days IC50 = 12.5 μM 27810589
LNCAP Antiproliferative activity assay 3 days IC50 = 12.5 μM 29117897
LNCaP Antagonist activity assay 144 h GI50 = 18.88 μM 28272894
LNCaP-AR Growth inhibition assay 144 h GI50 = 18.9 μM 25121586
C4-2B Antiproliferative activity assay 12 h IC50 = 20.77 μM 29758518
A31 Growth inhibition assay 72 h GI50 = 27.5 μM 28011219
22Rv1 Antiproliferative activity assay 96 h IC50 = 31.76 μM 27301368
22Rv1 Antiproliferative activity assay 96 h IC50 = 31.76 μM 26965862
DU145 Antiproliferative activity assay 96 h IC50 = 32.27 μM 27301368
LNCAP Antiproliferative activity assay 72 h IC50 = 33.84 μM 29448139
CW22Rv1 Antagonist activity assay 72 h IC50 = 35.75 μM 28272894
22Rv1 Antiproliferative activity assay 72 h IC50 = 36.66 μM 29448139
22Rv1 Antiproliferative activity assay 12 h IC50 = 36.66 μM 29758518
LNCAP Antiproliferative activity assay 12 h IC50 = 42.37 μM 29758518
DU145 Antiproliferative activity assay 3 days IC50 = 46.1 μM 27810589
DU145 Antiproliferative activity assay 3 days IC50 = 46.1 μM 29117897
LNCAP/AR Antagonist activity assay IC50 = 0.021 μM 27717544
MDA-MB-453 Antagonist activity assay EC50 = 0.049 μM 23713567
LNCAP Growth inhibition assay GI50 = 0.12 μM 28011219
LNCAP Growth inhibition assay GI50 = 2.88 μM 25634130
CWR22Rv1 Growth inhibition assay GI50 = 3.34 μM 25634130
PC3 Growth inhibition assay GI50 = 9.15 μM 25634130
他の多くの細胞株試験データをご覧になる場合はこちらをクリックして下さい

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。
Targets
Androgen Receptor [1]
(LNCaP cells)
36 nM
In Vitro
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 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]
Kinase Assay 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.
細胞実験 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.
実験結果図 Methods Biomarkers 結果図 PMID
Western blot AR / ERG / NOTCH1 / PSA / Cleaved PARP1 / Cleaved caspase 7 AR-FL / AR-v7 / pAR(S213) / pAkt(S473) / pMdm2(S166) CXCR7 28607007
Growth inhibition assay Cell proliferation 28115200
Immunofluorescence AR pAKT(S473) CXCR7 27588408
ELISA osteoprotegerin 27015557
In Vivo
In Vivo Enzalutamide induces great tumor regression in castrate male mice bearing LNCaP/AR xenografts at a dose of 10 mg/kg. [1]
動物実験 動物モデル Castration-resistant LNCaP/HR xenografts in male SCID mice
投与量 10 mg/kg
投与経路 Administered via gavage daily
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05339672 Recruiting
Drug-drug Interaction
Radboud University Medical Center|Astellas Pharma Inc
July 1 2024 --
NCT06130995 Not yet recruiting
Androgen Deprivation Therapy|Locally Advanced Prostate Cancer
University of Oklahoma
January 2024 Phase 1
NCT06096870 Not yet recruiting
Prostate Cancer|Recurrent Prostate Cancer|PET Positive
National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)
January 12 2024 Phase 2
NCT05743621 Not yet recruiting
Prostatic Neoplasms Castration-Resistant
Weill Medical College of Cornell University|Sagimet Biosciences Inc.
April 2023 Phase 1

化学情報

分子量 464.44 化学式

C21H16F4N4O2S

CAS No. 915087-33-1 SDF Download Enzalutamide SDFをダウンロードする
Smiles CC1(C(=O)N(C(=S)N1C2=CC(=C(C=C2)C(=O)NC)F)C3=CC(=C(C=C3)C#N)C(F)(F)F)C
保管

In vitro
Batch:

DMSO : 92 mg/mL ( (198.08 mM); 吸湿したDMSOは溶解度を減少させます。新しいDMSOをご使用ください。)

Ethanol : 24 mg/mL

Water : Insoluble

モル濃度計算器

in vivo
Batch:

Add solvents to the product individually and in order.

投与溶液組成計算機

実験計算

モル濃度計算器

質量 濃度 体積 分子量

投与溶液組成計算機(クリア溶液)

ステップ1:実験データを入力してください。(実験操作によるロスを考慮し、動物数を1匹分多くして計算・調製することを推奨します)

mg/kg g μL

ステップ2:投与溶媒の組成を入力してください。(ロット毎に適した溶解組成が異なる場合があります。詳細については弊社までお問い合わせください)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結果:

投与溶媒濃度: mg/ml;

DMSOストック溶液調製方法: mg 試薬を μL DMSOに溶解する(濃度 mg/mL, 注:濃度が当該ロットのDMSO溶解度を超える場合はご連絡ください。 )

投与溶媒調製方法:Take μL DMSOストック溶液に μL PEG300,を加え、完全溶解後μL Tween 80,を加えて完全溶解させた後 μL ddH2O,を加え完全に溶解させます。

投与溶媒調製方法:μL DMSOストック溶液に μL Corn oil,を加え、完全溶解。

注意:1.ストック溶液に沈殿、混濁などがないことをご確認ください;
2.順番通りに溶剤を加えてください。次のステップに進む前に溶液に沈殿、混濁などがないことを確認してから加えてください。ボルテックス、ソニケーション、水浴加熱など物理的な方法で溶解を早めることは可能です。

技術サポート

ストックの作り方、阻害剤の保管方法、細胞実験や動物実験の際に注意すべき点など、製品を取扱う時に問い合わせが多かった質問に対しては取扱説明書でお答えしています。

Handling Instructions

他に質問がある場合は、お気軽にお問い合わせください。

* 必須

大学・企業名を記入してください
名前を記入してください
電子メール・アドレスを記入してください 有効なメールアドレスを入力してください
お問い合わせ内容をご入力ください
Tags: Enzalutamideを買う | Enzalutamide ic50 | Enzalutamide供給者 | Enzalutamideを購入する | Enzalutamide費用 | Enzalutamide生産者 | オーダーEnzalutamide | Enzalutamide化学構造 | Enzalutamide分子量 | Enzalutamide代理店