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Formula | C26H29NO.C6H8O7 |
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Molecular Weight | 563.64 | CAS No. | 54965-24-1 | |
Solubility (25°C)* | In vitro | DMSO | 100 mg/mL (177.41 mM) | |
Ethanol | 100 mg/mL (177.41 mM) | |||
Water | Insoluble | |||
* <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. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | 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. | |
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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] |
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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%. [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] |
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Animal Study: |
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, , University of North Texas Health Science Center, 2014.
Mcam stabilizes luminal progenitor breast cancer phenotypes via Ck2 control and Src/Akt/Stat3 attenuation [ bioRxiv, 2024, 2023.05.10.540211] | PubMed: 38562809 |
Generation of a new Adar1p150 - /- mouse demonstrates isoform-specific roles in embryonic development and adult homeostasis [ RNA, 2023, 29(9):1325-1338.] | PubMed: 37290963 |
Generation of a new Adar1p150-/- mouse demonstrates isoform-specific roles in embryonic development and adult homeostasis [ RNA, 2023, rna.079509.122] | PubMed: 37290963 |
Over-expression of ADAR1 in mice does not initiate or accelerate cancer formation in vivo [ NAR Cancer, 2023, 5(2):zcad023] | PubMed: 37275274 |
Over-expression of ADAR1 in mice does not initiate or accelerate cancer formation in vivo [ NAR Cancer, 2023, 5(2):zcad023] | PubMed: 37275274 |
Bacterial diet modulates tamoxifen-induced death via host fatty acid metabolism [ Nat Commun, 2022, 13(1):5595] | PubMed: 36151093 |
Srsf2P95H/+ co-operates with loss of TET2 to promote myeloid bias and initiate a chronic myelomonocytic leukemia-like disease in mice [ Leukemia, 2022, 10.1038/s41375-022-01727-6] | PubMed: 36271153 |
Nuclear FGFR1 Regulates Gene Transcription and Promotes Antiestrogen Resistance in ER+ Breast Cancer [ Clin Cancer Res, 2021, 10.1158/1078-0432.CCR-20-3905] | PubMed: 34011560 |
USP35, regulated by estrogen and AKT, promotes breast tumorigenesis by stabilizing and enhancing transcriptional activity of estrogen receptor α [ Cell Death Dis, 2021, 12(6):619] | PubMed: 34131114 |
Collagen I Fibrous Substrates Modulate the Proliferation and Secretome of Estrogen Receptor-Positive Breast Tumor Cells in a Hormone-Restricted Microenvironment [ ACS Biomater Sci Eng, 2021, 10.1021/acsbiomaterials.0c01803] | PubMed: 33688723 |
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