Tamoxifen

製品コードS1238 バッチS123804

印刷

化学情報

Chemical Structure Synonyms ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen Storage
(From the date of receipt)		 2 years 4°C, in dark and seal
化学式

C26H29NO
分子量 371.51 CAS No. 10540-29-1
Solubility (25°C)* 体外 Ethanol 74 mg/mL (199.18 mM)
DMSO (warmed with 50ºC water bath) 10 mg/mL (26.91 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%absolute ethyl alcohol 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。

 5.000mg/ml (13.46mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clear absolute ethyl alcohol 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 Tamoxifenは、エストロゲンアゴニスト作用とアンタゴニスト作用の両方を示す、経口活性型の選択的エストロゲン受容体モジュレーター(SERM)です。Tamoxifenは乳房細胞におけるエストロゲンの作用を阻害し、骨、肝臓、子宮細胞などの他の細胞ではエストロゲン活性を活性化させることができます。Tamoxifenは強力なHSP90活性化因子であり、HSP90分子シャペロンのATPase活性を高めます。
in vitro

TAM treatment inhibits significantly MCF7 cell proliferation. Low doses of this compound are able to induce structural chromosomal aberrations (deletions, isochromosomes, translocations, and dicentric chromosomes) in both ER+ and ER- breast cancer cells. This genotoxic effect is higher in those cell lines with HER2 gene amplification. Whereas this chemical at lower concentrations (0.1-1 μM) induces a cell-cycle arrest, pharmacological concentrations (above 5 μM) of TAM have been found to induce apoptosis of breast cancer cells. 5 μM TAM rapidly induced sustained activation of ERK1/2 in ER-positive breast cancer cell lines (MCF-7 and T47D)
in vivo

Tamoxifen (TAM) is widely used for both treatment and prevention of breast cancer. However, it is also carcinogenic in human uterus and rat liver. Tm-inducible Cre-loxP systems are being used in broad areas of research and are providing important biologic insights in tissue development, maintenance, and function. This compound-induced nuclear localization of Cre recombinase is time- and dose-dependent. Higher doses of this chemical induce recombination weeks following administration and lower doses of it induce recombination up to one week following administration. Duration of its-induced gene recombination is also dose-dependent. Administration of high Tm doses leads to extended CreER nuclear localization. Tm treatment induces side effects that may have physiologic consequences in Tm-inducible models.

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF7 and T47D
濃度 10-6 mol/L
反応時間 24, 48, and 96 h
実験の流れ

48 h before the addition of E2 and TAM, cells were washed with 5 mL phosphate-buffered saline (PBS) and then switched to phenol red-free RPMI-1640 containing 10% charcoal-stripped FBS. E2 and this compound were dissolved in absolute ethanol and diluted in the media at 10-8 mol/L and 10-6 mol/L, respectively, and then added to the culture medium at 24, 48, and 96 h.
動物実験 動物モデル Pdx1PB-CreERTm mice
投薬量 --
投与方法 s.c.

参考

  • https://pubmed.ncbi.nlm.nih.gov/711743/
  • https://pubmed.ncbi.nlm.nih.gov/27357940/
  • https://pubmed.ncbi.nlm.nih.gov/17363451/
  • https://pubmed.ncbi.nlm.nih.gov/22470452/
  • https://pubmed.ncbi.nlm.nih.gov/10963646/
  • https://pubmed.ncbi.nlm.nih.gov/20376192/
  • https://pubmed.ncbi.nlm.nih.gov/15175332/
  • https://pubmed.ncbi.nlm.nih.gov/9828250/

カスタマーフィードバック

, , Oncotarget, 2015, 6(4):2315-30.

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：

Landscape of gene fusions in hormone receptor-positive breast cancer reveals ADK fusions as drivers of progression and potential therapeutic targets [ Cell Discov, 2025, 11(1):89] PubMed: 41213951
Tamoxifen induces PI3K activation in uterine cancer [ Nat Genet, 2025, 57(9):2192-2202] PubMed: 40846762
The integrated stress response fine-tunes stem cell fate decisions upon serine deprivation and tissue injury [ Cell Metab, 2025, 37(8):1715-1731.e11] PubMed: 40513561
Medium from human iPSC-derived primitive macrophages promotes adult cardiomyocyte proliferation and cardiac regeneration [ Nat Commun, 2025, 16(1):3012] PubMed: 40148355
SGK1 drives hippocampal demyelination and diabetes-associated cognitive dysfunction in mice [ Nat Commun, 2025, 16(1):1709] PubMed: 39962079
Cold exposure promotes the progression of osteoarthritis through downregulating APOE in cartilage [ EMBO Mol Med, 2025, 17(8):2137-2162] PubMed: 40664892
Nur77 attenuates Paneth cell necroptosis-induced intestinal inflammation through regulating endoplasmic reticulum homeostasis in sepsis [ J Adv Res, 2025, S2090-1232(25)00582-X] PubMed: 40749794
Targeting estrogen-regulated system xc- promotes ferroptosis and endocrine sensitivity of ER+ breast cancer [ Cell Death Dis, 2025, 16(1):30] PubMed: 39833180
CDC20 protects the heart from doxorubicin-induced cardiotoxicity by modulating CCDC69 degradation [ Cell Mol Biol Lett, 2025, 30(1):29] PubMed: 40045239
Intestinal overexpression of Pla2g10 alters the composition, diversity and function of gut microbiota in mice [ Front Cell Infect Microbiol, 2025, 15:1535204] PubMed: 40160470

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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。

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