Tamoxifen Citrate

SKU: orb1310249

Description

Tamoxifen Citrate is an orally active SERM that antagonizes estrogen in breast tissue while acting as an agonist in bone, liver, and uterus. It functions as an Hsp90 activator to induce autophagy and apoptosis, and is widely used in research for generating conditional knockout models in CreER(T2) mice and studying liver injury.

Research Area

Cell Biology, Metabolism Research, Signal Transduction

Images & Validation

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Key Properties

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CAS Number	54965-24-1
MW	563.65
Purity	99.86% (May vary between batches)
Formula	C₃₂H₃₇NO₈
SMILES	CC/C(=C(\c1ccccc1)/c1ccc(cc1)OCCN(C)C)/c1ccccc1.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
Target	Autophagy,Estrogen/progestogen Receptor,HSP,Apoptosis,Estrogen Receptor/ERR
Solubility	10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (3.55 mM);DMSO:50 mg/mL (88.71 mM);Ethanol:2.8 mg/mL (4.97 mM)

Bioactivity

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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 (Tpot) (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 Tpot of 2.3 days, and a %LI of 23%. 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. Read more...
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. 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. 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. 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). Read more...
Cell Research	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. (Only for Reference) Read more...

Storage & Handling

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Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

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chaperone, (Z)-Tamoxifen, Apoptosis, Autophagy, modulator, Estrogen Receptor/ERR, EstrogenReceptor, HSP, Hsp90, estrogen, Estrogen Receptor, ERR, ER, ICI 46474 Citrate, ICI46474, ICI-46474, ICI46474 Citrate, ICI-46474 Citrate, trans-Tamoxifen, uterine, Tamoxifen, Tamoxifen Citrate, Tamoxifen Z-isomer citrate, progestogen Receptor, progestogenReceptor, SERM

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Compound Identifiers

PubChem CID

2733525 ↗

Key Properties

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No computed properties available.

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