Tamoxifen

製品コードS1238 バッチS123803

印刷

化学情報

Chemical Structure Synonyms ICI 46474, (Z)-Tamoxifen, trans-Tamoxifen Storage
(From the date of receipt)		 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) 7.5 mg/mL (20.18 mM)
Water Insoluble
体内 （毎回新しく調製した物を用意してください）
Clear solution
10%DMSO 40%PEG300 5%Tween80 45%ddH2O
0.75mg/ml Taking the 1 mL working solution as an example, add 100 μL of 7.5 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 450 μL of ddH2O to make it clear. Volume up to 1 mL. 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 is an orally active, selective estrogen receptor modulator (SERM) which exhibits both estrogenic agonist and antagonist effects. It blocks estrogen action in breast cells and can activate estrogen activity in other cells, such as bone, liver, and uterine cells. Tamoxifen is a potent Hsp90 activator and enhances the Hsp90 molecular chaperone ATPase activity.
in vitro

TAM treatment inhibits significantly MCF7 cell proliferation. Low doses of TAM 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[2]. Whereas TAM 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)[3]
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[2]. 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. Tamoxifen-induced nuclear localization of Cre recombinase is time- and dose-dependent. Higher doses of tamoxifen induce recombination weeks following administration and Lower doses of tamoxifen induce recombination up to one week following administration. Duration of tamoxifen-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[4].

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 TAM 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.

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：

Therapeutic targeting nudix hydrolase 1 creates a MYC-driven metabolic vulnerability [ Nat Commun, 2024, 15(1):2377] PubMed: 38493213
Single cell profiling of female breast fibroadenoma reveals distinct epithelial cell compositions and therapeutic targets [ Nat Commun, 2023, 10.1038/s41467-023-39059-3] PubMed: 37328469
CircRREB1 mediates lipid metabolism related senescent phenotypes in chondrocytes through FASN post-translational modifications [ Nat Commun, 2023, 14(1):5242] PubMed: 37640697
Single cell profiling of female breast fibroadenoma reveals distinct epithelial cell compositions and therapeutic targets [ Nat Commun, 2023, 14(1):3469] PubMed: 37328469
CircRREB1 mediates lipid metabolism related senescent phenotypes in chondrocytes through FASN post-translational modifications [ Nat Commun, 2023, 14(1):5242] PubMed: 37640697
Dlg1 deletion in microglia ameliorates chronic restraint stress induced mice depression-like behavior [ Front Pharmacol, 2023, 14:1124845] PubMed: 36909184
Using a Quantitative High-Throughput Screening Platform to Identify Molecular Targets and Compounds as Repurposing Candidates for Endometriosis [ Biomolecules, 2023, 13(6)965] PubMed: 37371546
Carbonic Anhydrase Inhibitors Induce Ferroptosis through Inhibition of AKT/FTH1 Signaling in Ewing Sarcoma Tumor Cells [ Cancers (Basel), 2023, 10.3390/cancers15215225] PubMed: 37958399
Mechanical manipulation of cancer cell tumorigenicity via heat shock protein signaling [ Sci Adv, 2023, 9(27):eadg9593] PubMed: 37418519
RECOVER identifies synergistic drug combinations in vitro through sequential model optimization [ Cell Rep Methods, 2023, 3(10):100599] PubMed: 37797618

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