Mifepristone

別名:RU486, C-1073, RU 38486, RU-486

Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.

Mifepristone化学構造

CAS No. 84371-65-3

サイズ 価格(税別) 在庫状況
10mM (1mL in DMSO) JPY 40100 国内在庫あり
JPY 13300 国内在庫あり
JPY 33500 国内在庫あり
JPY 75500 国内在庫なし(納期7~10日)

代表番号: 045-509-1970|電子メール:[email protected]
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カスタマーフィードバック1个实验数据

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Mifepristone関連製品

Estrogen/progestogen Receptor阻害剤の選択性比較

Cell Data

Cell Lines Assay Type Concentration Incubation Time 活性情報 PMID
T47D-C124 cells Function assay 24 h Antagonist activity at progesterone receptor in human T47D-C124 cells transfected with luciferase gene linked to MMTV promoter assessed as inhibition of progesterone-induced luciferase transactivation activity after 24 hrs, IC50=2.1e-05 μM 19216549
T47D cells Function assay 48 h Antagonist activity at progesterone receptor in human T47D cells assessed as inhibition of progesterone-induced alkaline phosphatase activity after 48 hrs, IC50=4.5e-05 μM 19216549
A549 cells Function assay 16 h Antagonist activity at glucocorticoid receptor in human A549 cells assessed as inhibition of corticoid-induced transcription after 16 hrs by glucocorticoid response element-driven luciferase reporter gene assay, IC50=0.0016 μM 19217285
rat H4-IIE cells Function assay 1 h Antagonist activity against glucocorticoid receptor in rat H4-IIE cells assessed as inhibition of dexamethasone-induced receptor transactivation pre-incubated for 1 hr before dexamethasone addition and measured 24 hrs post dexamethasone stimulation by tyrosine aminotransferase enzyme assay, IC50=0.00194 μM 26218343
human K562/R7 cells Function assay 72 h Potentiation of doxorubicin-induced cytotoxicity against doxorubicin-resistant human K562/R7 cells assessed as doxorubicin IC50 at 1 uM after 72 hrs by MTT assay, IC50=0.9 μM 25634041
CHO-K1 cells Function assay Inhibition of CHO-K1 cells expressing glucocorticoid receptor, IC50=8e-06 μM 15456242
neuroblastoma cells Function assay In vitro antagonist potency in transactivation assay in neuroblastoma cells expressing human PR-B progesterone receptor, IC50=2.5e-05 μM 11150172
CV-1 cells Function assay Antagonistic activity against human progesterone receptor B (hPR-B) in co-transfected CV-1 cells, IC50=0.00018 μM 9484511
HEK293 cells Function assay Antagonist activity against glucocorticoid receptor (unknown origin) expressed in HEK293 cells by GRE-dependent luciferase reporter gene assay, IC50=0.000298 μM 26218343
COS7 cells Function assay Antagonist activity at cloned glucocorticoid receptor-ligand binding domain expressed in african green monkey COS7 cells by GAL4 luciferase reporter assay, IC50=0.0006 μM 18504132
SW1353 cells Function assay Binding affinity to glucocorticoid receptor in SW1353 cells by whole-cell binding assay, Ki=0.00082 μM 17822897
A549 cells Function assay Antagonist activity at human glucocorticoid receptor assessed as inhibition of corticoid-induced transcription in human A549 cells by GRE-linked luciferase reporter gene assay, IC50=0.0016 μM 17317167
HeLa cells Function assay Effective concentration against inhibition of Dexamethasone induced glucocorticoid receptor transactivation of mouse mammary tumor virus luciferase gene in HeLa cells, EC50=0.002 μM 16112571
NIH3T3 cells Function assay In vitro antagonist potency in transactivation assay in NIH3T3 cells expressing glucocorticoid receptor, IC50=0.0022 μM 11150172
CHO cells Function assay Inhibition of Dexamethasone stimulated transcriptional activity in CHO cells expressing glucocorticoid receptor, IC50=0.005 μM 12824023
hGRAF cells Function assay Inhibition of human GR expressed in hGRAF cells, Ki=0.005 μM 17070047
COS-1 Function assay Binding affinity for human androgen receptor in transiently-transfected COS-1 cells, Ki=0.022 μM 9484511
rat hepatocytes Function assay Inhibition of dexamethasone-induced GR-mediated tyrosine amino transferase activity in rat hepatocytes, IC50=0.27 μM 15261266
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生物活性

製品説明 Mifepristone is a remarkably active antagonist of progesterone receptor and glucocorticoid receptor with IC50 of 0.2 nM and 2.6 nM, respectively. Mifepristone promotes cell autophagy and apoptosis, decreases Bcl-2 level and increases Beclin1 level, accompanied by weakened interaction between Bcl-2 and Beclin1.
特性 Mifepristone is the first approved medication for patients with endogenous cushing
Targets
Bcl-2 [5] Progesterone receptor [1]
(T47D cells)
Glucocorticoid receptor [1]
(A549 cells)
0.2 nM 2.6 nM
In Vitro
In vitro

Mifepristone inhibit corticoid-induced transcription from a glucocorticoid response element (GRE)-linked luciferase reporter gene in the human lung carcinoma cell line A549. Moreover, Mifepristone also blocks progesterone induction of alkaline phosphatase activity in the human breast cancer cell line T47D. [1] Mifepristone inhibits ovarian cancer cell growth of SK-OV-3 and OV2008 with IC50 of 6.25 μM and 6.91 μM, respectively. [2] A recent study shows that Mifepristone induces caspase-1 over expression both in differentiated and undifferentiated caspase-1-embryonic stem cells. [3]

Kinase Assay Glucocorticoid receptor (GR) antagonist activity, Progesterone receptor (PR) antagonist activity
T47D alkaline phosphatase assay: T47D human breast cancer cells are plated in 96-well tissue culture plates at 104 cells per well in assay medium [RPMI medium without phenol red containing 5% (v/v) charcoal-treated FBS and 1% (v/v) penicillin–streptomycin]. Two days later, the medium is decanted and Mifepristone or control is added at a final concentration of 0.1% (v/v) dimethylsulfoxide in fresh assay medium. Twenty-four hours later, an alkaline phosphatase assay is performed using a SEAP kit. The medium is decanted and the cells are fixed for 30 minutes at room temperature with 5% (v/v) formalin. The cells are washed once at room temperature with Hanks
細胞実験 細胞株 OV2008 and SK-OV-3 cells
濃度 0-20 μM
反応時間 24 hours
実験の流れ

Cell growth is evaluated in various ovarian cancer cell lines that are subjected to dose-response or time course treatments. Media containing each of the doses of fresh steroids is replaced every 24 hours. Control groups of cells are treated with vehicle ethanol at a final concentration of less than 0.05%. Number of viable cells is evaluated by trypsinization and counting in a hemocytometer chamber using trypan blue dye exclusion. Experiments are conducted in media without phenol red and supplemented with charcoal extracted fetal bovine serum, or media containing unextracted serum and having phenol red. Similar results are obtained with both media preparations; therefore, after performing the growth curves, all subsequent experiments are conducted using media with unextracted serum and in the presence of phenol red. When indicated, the proliferation IC50s are calculated using software designed to study drug interaction.

実験結果図 Methods Biomarkers 結果図 PMID
Western blot p-AKT / AKT / p-ERK / ERK MMP-2 / MMP-9 / COX-2 / VEGF 28938623
In Vivo
In Vivo

Mifepristone can impair the growth of SK-OV-3 tumors in immunosuppressed mice at 0.5 mg/day and 1 mg/day. [2] Mifepristone inhibits the prostate weight significantly in the highest doses in vivo, and inhibits growth of the prostate gland produced by dihydrotestosterone (DHT) to a greater extent than the induction of atrophy and cell death in rats. [4]

動物実験 動物モデル SK-OV-3 ovarian cancer cells are injected into immunosuppressed mice.
投与量 0.5 or 1 mg/day
投与経路 Implanted s.c. with pellets
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05177510 Recruiting
Labor Induced
Chelsea and Westminster NHS Foundation Trust
August 25 2023 Phase 3
NCT04905251 Recruiting
Medical Abortion
Linepharma International LTD
February 22 2022 --
NCT05062174 Withdrawn
BRCA1 Mutation|High-grade Serous Ovarian Cancer|TNBC - Triple-Negative Breast Cancer
Indiana University|Breast Cancer Research Foundation
November 1 2021 --
NCT04588688 Terminated
Central Adrenal Insufficiency|Mifepristone
Tobias Else|Corcept Therapeutics|University of Michigan
May 5 2021 Phase 2
NCT03659045 Completed
Abortion-Related Disorders
Assistance Publique Hopitaux De Marseille
January 15 2019 Not Applicable
NCT03258372 Completed
Healthy
Corcept Therapeutics
August 16 2017 Phase 1

化学情報

分子量 429.59 化学式

C29H35NO2

CAS No. 84371-65-3 SDF Download Mifepristone SDFをダウンロードする
Smiles CC#CC1(CCC2C1(CC(C3=C4CCC(=O)C=C4CCC23)C5=CC=C(C=C5)N(C)C)C)O
保管

In vitro
Batch:

DMSO : 85 mg/mL ( (197.86 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 : 85 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。

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