Tamoxifen Citrate

別名：ICI 46474, Istubal

製品コード：S1972 純度：99.99%

Tamoxifen Citrate is a selective estrogen receptor modulator (SERM). Tamoxifen Citrate is also a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity. Tamoxifen induces apoptosis and autophagy.

CAS No. 54965-24-1

サイズ	価格(税別)	在庫状況
10mM (1mL in DMSO)	JPY 29500	国内在庫あり
250mg	JPY 22000	国内在庫あり
1g	JPY 44500	国内在庫あり

代表番号: 045-509-1970\|電子メール：sales@selleck.co.jp よく尋ねられる質問

文献中Selleckの製品使用例（21）

1/2

カスタマーフィードバック1例

製品安全説明書

現在のバッチを見る：純度： 99.99%

99.99

Tamoxifen Citrate関連製品

関連ターゲット	Estrogen receptor Progesterone receptor ERR	もっと見る
関連製品	Cholesterol Endoxifen HCl G15 Licochalcone A AZD9496 PHTPP Liquiritigenin Brilanestrant (GDC-0810) Pregnenolone Estriol Lasofoxifene Tartrate Equol Genistin (Genistoside) Erteberel (LY500307) Elacestrant (RAD1901) Dihydrochloride GSK5182	もっと見る
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

阻害剤	Citation	Estrogen receptor	Progesterone receptor
Gestodene	0		✔
Pregnenolone	4		✔
Estriol	1	✔

1. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation. 2. "✔" indicates inhibitory effect, but without specific value.

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	活性情報	PMID
MCF7	Antiproliferative assay	3 mg/kg	48 hrs	Antiproliferative activity against MCF7 cells at 3 mg/kg/day after 48 hrs, IC50=5.09μM	16979337
HeLa	Function assay	1 uM	48 hrs	Antagonist activity at human ERalpha expressed in human HeLa cells coexpressing ERE-E1b-Luc assessed as inhibition of estradiol-induced transcriptional activation at 1 uM after 48 hrs by luciferase reporter gene assay	20621492
MCF7	Cytotoxicity assay	6 uM	96 hrs	Cytotoxicity against human MCF7 cells assessed as reduction of cell proliferation at 6 uM after 96 hrs by MTT assay	20621492
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

Targets

ER ^[1]
(Cell-free assay)

In Vitro
In vitro	Tamoxifen displays antitumor effect due to its antiestrogenic activity (ER). Values for the apparent affinity of Tamoxifen for the ER range between 30 and 0.01% of that obtained for estradiol, dependent on different ER source (species), protein concentration and condition used for assay. Binding of Tamoxifen to ER further leads to inhibition expression of estrogen-regulated genes, including growth factors and angiogenic factors secreted by the tumor that may stimulate growth by autocrine or paracrine mechanisms. Tamoxifen also directly induces programmed cell death. ^[1] Tamoxifen produces an inhibitory effect on MCF-7 cell [³H]thymidine incorporation and DNA polymerase activity as well as causing a reduction in DNA content of cultures and cell numbers. This inhibitory effect of Tamoxifen on MCF-7 cell growth can be readily reversed by addition of estradiol to the culture medium. 2 and 6 μM Tamoxifen reduces the proportion of cells in S phase and increases the number of cells in G1. At 10 μM, Tamoxifen causes cell death within 48 hr. ^[2] Tamoxifen inhibits MCF-7 growth with IC50 of ~10 nM after 10 days treatment. Tamoxifen inhibits plasminogen activator activity of MCF-7, and suppresses estradiol-stimulation of plasminogen activator activity. Tamoxifen also evokes minimal increases in cellular progesterone receptor levels. ^[3] Tamoxifen is able to inhibit the growth of prostate cancer cell PC3, PC3-M, and DU145 with IC50 ranged from 5.5-10 μM, which is related to its inhibition of protein kinase C and induction of p21(waf1/cip1). ^[4]
Kinase Assay	Competitive binding assays
Kinase Assay	Cells are harvested from 150-sq cm T-flasks, and cytosol is prepared at a protein concentration of approximately 2 mg/mL in phosphate buffer. Aliquots of this 180,000 ×g supernatant are then incubated with various concentrations of Tamoxifen and 2.5 nM [³H]estradiol for 16 hr at 0-4 ℃. The free steroids are absorbed by dextran-charcoal [l0 μL of 0.5% Dextran C-5% Norite A in TE buffer] for 1 hr at 0 ℃, and aliquots are counted after centrifugation at 800 ×g, 30 min. The relative binding ability of each competitor is taken as the ratio of the concentration of radioinert estradiol/competitor required to inhibit one-half of the specific [³H]estradiol binding, with the affinity of estradiol set at 100%.
細胞実験	細胞株	Human breast cancer cells MCF-7
	濃度	~1 μM
	反応時間	10 days
	実験の流れ	MCF-7 cells are seeded into T-25 flasks (1.5×10⁵ cells/flask) and grown for 2 days in the MEM supplemented with 10 mM HEPES buffer, gentamicin (50 μg/mL), penicillin (100 units/mL), streptomycin (0.1 mg/mL), bovine insulin (6 ng/mL), hydrocortisone (3.75 ng/mL), and 5% calf serum that has been treated with dextran-coated charcoal for 45 min at 55 ℃ to remove endogenous hormones. The medium is then changed to MEM supplemented as described above, except that it contains 2% charcoal dextran-treated calf serum and various concentrations of Tamoxifen. At the end of incubation, cell numbers are counted.
実験結果図	Methods	Biomarkers	結果図	PMID
	Western blot	p-AKT / AKT ER-α66 / ER-α36 / HER2 / EGFR p-AMPK / AMPK / p-ACC / ACC / p-P70S6K / p-S6 / p-4EBP1 CD36 / p-ERK / ERK		30759864
	Immunofluorescence	CD36		30573731

In Vivo
In Vivo	Tamoxifen administration to rapidly growing, estradiol-stimulated MCF-7 xenografts results in a dose-dependent retardation or cessation of tumor growth by significantly decreasing tumor cell proliferation in tumor. Tamoxifen treatment results in a slowing of tumor growth (tumor doubling time, 12 days), a significant increase in tumor potential doubling time (T_pot) (6.6 days), and a decrease in labeling index (%LI) (to 8%) by 23 days posttreatment, compared with untreated mice which shows a volume doubling time of 5 days, a T_pot of 2.3 days, and a %LI of 23%. ^[5] Tamoxifen has not only antiestrogenic but also estrogenic properties depending on the species, tissue, and gene. Tamoxifen displays favorable effects on bone and serum lipid concentrations and stimulation endometrium. ^[1]
動物実験	動物モデル	Human breast carcinoma xenografts MCF-7
	投与量	2 cm Tamoxifen capsules
	投与経路	Subcutaneous implantation

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試験 (data from https://clinicaltrials.gov, updated on 2024-05-22)
NCT06154590	Not yet recruiting	Metastatic Breast Cancer\|Tumor\|Muscle Neoplasms\|Chronic Pain	DR. DIANE CHISESI NFS. MD. PHD.\|IRB\|Paradyne Networks A Foundation	July 2024	--
NCT05156892	Recruiting	Ovarian Cancer	Anthony Joshua FRACP\|Royal Prince Alfred Hospital Sydney Australia\|Concord Hospital\|Prince of Wales Hospital Sydney\|St Vincent''s Hospital Sydney	September 4 2022	Phase 1
NCT04200066	Withdrawn	Glioblastoma\|Brain Tumor	University of Rochester	June 1 2022	Phase 1
NCT05133674	Unknown status	Breast Cancer\|Breast Carcinoma\|Breast Tumors\|Cancer of Breast\|Malignant Neoplasm of Breast	Karolinska University Hospital	April 4 2022	Phase 2

参考
[1] Osborne CK. N Engl J Med, 1998, 339(22), 1609-1618. [2] Furr BJ, et al. Pharmacol Therm, 1984, 25(2), 127-205. [3] Katzenellenbogen BS, et al. Cancer Res, 1984, 44(1), 112-119. [4] Rohlff C, et al. Prostate, 1998, 37(1), 51-59. [5] Sarkaria JN, et al. Cancer Res, 1993, 53(18), 4413-4417. [6] C K Osborne, et al. J Clin Oncol . 2000 Sep;18(17):3172-86. + 展開

参考

+ 展開

化学情報

分子量	563.64	化学式	C₂₆H₂₉NO.C₆H₈O₇
CAS No.	54965-24-1	SDF	Download Tamoxifen Citrate SDFをダウンロードする
Smiles	CCC(=C(C1=CC=CC=C1)C2=CC=C(C=C2)OCCN(C)C)C3=CC=CC=C3.C(C(=O)O)C(CC(=O)O)(C(=O)O)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ケ月-20°Cin solvent

In vitro
Batch:

DMSO : 100 mg/mL ( (177.41 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 : 49 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
=	×	×

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。

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 大学・企業名を記入してください

* 名前 名前を記入してください

* 電子メール 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

電話番号

* 内容 お問い合わせ内容をご入力ください

よくある質問（FAQ）

質問1:
I am wondering if the Tamoxifen (product Cat # S1972) is a 4-hydroxy Tamoxifen form or just plain Tamoxifen Citrate?

回答
The Tamoxifen (S1972) is a prodrug, just plain Tamoxifen citrate.

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):