Mifepristone

別名：C-1073, RU 38486

製品コード：S2606 純度：99.95%

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.

CAS No. 84371-65-3

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 34500	国内在庫なし(納期7~10日)
50mg	JPY 22000	国内在庫あり
200mg	JPY 37000	国内在庫あり
1g	JPY 73500	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（28）

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製品安全説明書

現在のバッチを見る：純度： 99.95%

99.95

Mifepristone関連製品

関連ターゲット	Estrogen receptor Progesterone receptor ERR	もっと見る
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関連化合物ライブラリー	FDA-approved Drug Library Natural Product Library Bioactive Compound Library-I Exosome Secretion Related Compound Library Human Hormone Related Compound Library	もっと見る

シグナル伝達経路

Estrogen/progestogen Receptorシグナル伝達経路

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

Cell Data

Cell Lines	Assay Type	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

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
Kinase Assay	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 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
実験結果図	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
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06394999	Not yet recruiting	Female Contraception	Leiden University Medical Center\|Karolinska Institutet\|Women on Waves\|Children''s Investment Fund Foundation	September 2024	Phase 3
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

参考
[1] Jiang W, et al. Bioorg Med Chem, 2006, 14(19), 6726-6732. [2] Goyeneche AA, et al. Clin Cancer Res, 2007, 13(11), 3370-3379. [3] Wang Y, et al. Stem Cells, 2012, 30(2), 169-179. [4] Cabeza M, et al. J Steroid Biochem Mol Biol, 2007, 104(3-5), 321-325. [5] Lindong Zhang, et al. Biosci Rep. 2019 Jul 23;39(7):BSR20190094. + 展開

参考

+ 展開

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	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1年-80°Cin solvent
保管	3年-20°C粉	溶液の保管冷凍と解凍の繰り返しを避けるため小分けにしてください	1个月-20°Cin solvent

In vitro
Batch:

DMSO : 86 mg/mL ( (200.19 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 : 43 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
	Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	4.5mg/ml (10.48mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 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.	投与溶液組成計算機
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O	6.0mg/ml (13.97mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 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 make it clear; 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 1 95% Corn oil	0.53mg/ml (1.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 10.6 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.

実験計算

モル濃度計算器

質量	濃度	体積	分子量
=	×	×

希釈計算器分子量計算器

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）

投与量 mg/kg 動物平均体重 g 投与体積（動物毎）μL 動物数匹

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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