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Tamoxifen [10540-29-1]

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Referencia NB-64-36909-1g

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Marca : Neo Biotech

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Tamoxifen

(Synonyms: Z-Tamoxifen, trans-Tamoxifen, ICI47699) Copy Product Info

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Synonyms: Z-Tamoxifen, trans-Tamoxifen, ICI47699

Catalog No. T6906 Copy Product Info

Purity: 99.97%

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Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.

Cas No. 10540-29-1

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For research use only—not for human use. No sales to individuals. Use as intended only.

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Purity:99.97%

Color:White

Product Introduction

Bioactivity

Description	Tamoxifen is an orally active selective estrogen receptor modulator (SERM) that acts as an estrogen antagonist in breast cells and an agonist in bone, liver, and uterine cells. It can be used to induce gene knockout and liver injury models in mice, and also exhibits multiple biological activities, including activation of Hsp90, induction of autophagy and apoptosis, and inhibition of EBOV and MARV viral infections.
Targets & IC50	A2058 cells:12.5 μM (EC50), DU-145 cells:10.87 μM, FaDu cells:5.39 μM, A253 cells:8.92 μM, CHO cells:> 100 μM, A549 cells:1.86 μg/mL, B16 F10 cells:64.87 μM, 518A2 cells:7.62 μM, A2780 cells:7.77 μM, A431 cells:> 100 μM, Astrocytes:> 10 μM, DLD-1 cells:11.06 μM
In vitro	METHODS: Human breast cancer cells MCF-7 were treated with Tamoxifen (0.25-4 μM) for 24 h. Cell viability was measured using the CCK-8. RESULTS: Tamoxifen significantly inhibited the proliferation of MCF-7 cells in a dose-dependent manner. [1] METHODS: ER-negative breast cancer cells SK-BR3, MDA-MB-453, MDA-MB-468, MDA-MB-231, and HCC-1937 were treated with Tamoxifen (1-10 μM) for 24-36 h, and apoptosis was detected using Flow Cytometry. RESULTS: Tamoxifen induced apoptosis in MDA-MB-231, MDA-MB-468, MDA-MB-453 and SK-BR3 cells in a dose- and time-dependent manner, while no significant apoptotic effect was observed in HCC-1937 cells. [2]
In vivo	METHODS: To test the antitumor activity in vivo, Tamoxifen (100 mg/kg) was administered orally to NCr athymic nude mice bearing ER-negative breast cancer tumors MDA-MB-468 or HCC-1937 three times per week for four to five weeks. RESULTS: Tamoxifen significantly inhibited the growth of MDA-MB-468 tumors, whereas the growth of HCC-1937 tumors was not affected. [2] METHODS: To test the effect on mouse behavior, Tamoxifen (75 mg/kg in 10% ethanol+90% sunflower seed oil) was administered intraperitoneally to C57BL/6 mice once a day for seven days. RESULTS: Tamoxifen affects motor activity, socialization, and anxiety in mice. [3]
Synonyms	Z-Tamoxifen, trans-Tamoxifen, ICI47699
Disease Modeling Protocol	Conditional Genetic Engineering Disease Model Modeling Mechanism： Tamoxifen activates the AP-1 transcription factor (upregulating the expression of c-fos, c-jun, and ap1s1 by 3-7 times), driving the potent expression of MMP family genes (especially mmp9 and mmp13a) in skin epithelial cells (upregulated by 127-fold and 1145-fold, respectively). Excessive MMPs degrade the extracellular matrix, inducing skin epithelial cell cytotoxicity, apoptosis, and necrosis, ultimately leading to the tail necrosis phenotype. Related Products： Tamoxifen (T6906) Modeling Method： Experimental Subject： Zebrafish: Wild-type tropical 5D strain, secA5-YFP transgenic strain (visualisation of apoptosis). Embryonic stage (4–5 hpf post-eclosion), juvenile stage (48 hpf) to adult. Dosage and Administration Route： 1–15 μM tamoxifen (dissolved in 0.1% DMSO, final concentration) Static exposure in embryo medium Exposure by placing embryos/larvae individually in 96-well plates (containing 100 μL embryo medium); adult fish exposed directly to drug-containing medium Dosing Frequency and Duration Model： Embryonic stage: Continuous exposure from 6–120 hpf; Larval stage: Single 24-hour exposure at 48–72 hpf; Adult stage: Single 1.5-hour exposure Validation： Phenotypic validation: Specific necrosis appeared in the tail, which could extend to the pectoral fins and the entire skin of adult fish. Apoptotic signals (secA5-YFP) were spatiotemporally colocalized with the necrotic area. Molecular markers: qRT-PCR showed significant upregulation of genes such as mmp9, mmp13a, and igfbp1a. Immunohistochemistry confirmed high expression of MMP13a protein in the tail injury area. Specificity validation: Knockdown of ER inhibitors (G-15), p53 inhibitors (pifithrin α), and ER (esr1, esr2a, esr2b) morpholino did not improve the phenotype, while MMP inhibitors (EDTA, GM 6001, SR 11302) could completely or partially block the necrotic phenotype. Dose-relatedness: 1-5 μM had no obvious phenotype, ≥10 μM induced 100% tail necrosis, and 15 μM was accompanied by increased mortality. Precautions： References：Bugel SM,et,al. Phenotype anchoring in zebrafish reveals a potential role for matrix metalloproteinases (MMPs) in tamoxifen's effects on skin epithelium. Toxicol Appl Pharmacol. 2016 Apr 1;296:31-41.

Chemical Properties

Molecular Weight	371.51
Formula	C₂₆H₂₉NO
Cas No.	10540-29-1
Smiles	C(=C(/CC)\C1=CC=CC=C1)(\C2=CC=C(OCCN(C)C)C=C2)/C3=CC=CC=C3
Relative Density.	1.042 g/cm3

Storage & Solubility Information

Storage

Keep away from direct sunlight,Keep away from moisture Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 12.5 mg/mL (33.65 mM), Sonication is recommended.

Ethanol: 100 mg/mL (269.17 mM), Sonication and heating are recommended.

In Vivo Formulation

Corn oil: 40 mg/mL (107.67 mM), Sonication is recommended.

Please add the solvents sequentially, clarifying the solution as much as possible before adding the next one. Dissolve by heating and/or sonication if necessary. Working solution is recommended to be prepared and used immediately. The formulation provided above is for reference purposes only. In vivo formulations may vary and should be modified based on specific experimental conditions.

Solution Preparation Table

DMSO/Ethanol

	1mg	5mg	10mg	50mg
1 mM	2.6917 mL	13.4586 mL	26.9172 mL	134.5859 mL
5 mM	0.5383 mL	2.6917 mL	5.3834 mL	26.9172 mL
10 mM	0.2692 mL	1.3459 mL	2.6917 mL	13.4586 mL
20 mM	0.1346 mL	0.6729 mL	1.3459 mL	6.7293 mL

Ethanol

	1mg	5mg	10mg	50mg
50 mM	0.0538 mL	0.2692 mL	0.5383 mL	2.6917 mL
100 mM	0.0269 mL	0.1346 mL	0.2692 mL	1.3459 mL

Note : The dilution table applies only to solid products. For liquid products, please calculate the stock solution based on the stated concentration and/or density.

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In Vivo Formulation Calculator (Clear solution)

Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:

For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH₂O , the resulting working solution concentration would be 2 mg/mL.

Stock Solution Preparation:

Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.

Preparation of the In Vivo Formulation:

1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.

2) Add 50 µL Tween 80 and mix well until fully clarified.

3) Add 450 µL Saline,PBS or ddH₂O and mix thoroughly until a homogeneous solution is obtained.

This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.

All co-solvents required for this protocol, includingDMSO, PEG300/PEG400, Tween 80, SBE-β-CD, and Corn oil, are available for purchase on the TargetMol website.

Dose Conversion

Keywords

uterineTamoxifenSERMprogestogenReceptorprogestogen ReceptormodulatorliverICI-47699ICI-46474ICI46474ICI 47699Hsp90HSPEstrogenReceptorEstrogen Receptor/ERREstrogen ReceptorERRERchaperoneAutophagyATPaseApoptosis(Z)-Tamoxifen

Related Tags: Tamoxifen chemical structure | Tamoxifen in vivo | Tamoxifen in vitro | Tamoxifen formula | Tamoxifen molecular weight