Antibodies
Tamoxifen Citrate
- 貨號 Cat. No.
- S1972
- 規格 Size
- 10mM/1mLã€250mg
- 品牌 Brand
- Selleckchem
Description
Tamoxifen Citrate
Catalog No.S1972
Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding.
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Biological Activity
| Description | Tamoxifen Citrate is an antagonist of the estrogen receptor by competitive inhibition of estrogen binding. | |||||
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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] | |||||
| 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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Protocol(Only for Reference)
Kinase Assay: [3]
| Competitive binding assays | Cells are harvested from 150-sq cm T-flasks, and cytosol is prepared at a protein concentration of approximately 2 mg/mL in phosphate buffer. Aliquots of this 180,000 ×g supernatant are then incubated with various concentrations of Tamoxifen and 2.5 nM [3H]estradiol for 16 hr at 0-4 ℃. The free steroids are absorbed by dextran-charcoal [l0 μL of 0.5% Dextran C-5% Norite A in TE buffer] for 1 hr at 0 ℃, and aliquots are counted after centrifugation at 800 ×g, 30 min. The relative binding ability of each competitor is taken as the ratio of the concentration of radioinert estradiol/competitor required to inhibit one-half of the specific [3H]estradiol binding, with the affinity of estradiol set at 100%. |
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Cell Assay: [3]
| Cell lines | Human breast cancer cells MCF-7 |
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| Concentrations | ~1 μM |
| Incubation Time | 10 days |
| Method | 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. |
Animal Study: [5]
| Animal Models | Human breast carcinoma xenografts MCF-7 |
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| Dosages | 2 cm Tamoxifen capsules |
| Administration | Subcutaneous implantation |
| Solubility | 30% PEG400/0.5% Tween80/5% propylene glycol, 30 mg/mL |
References
Chemical Information
Download Tamoxifen Citrate SDF
| Molecular Weight (MW) | 563.64 |
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| Formula | C26H29NO.C6H8O7 |
| CAS No. | 54965-24-1 |
| Storage | 3 years -20℃Powder |
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| 6 months-80℃in DMSO | |
| Syonnyms | Istubal |
| Solubility (25°C) * | In vitro | DMSO | 100 mg/mL (177 mM) |
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| Water | <1 mg/mL (<1 mM) | ||
| Ethanol | <1 mg/mL (<1 mM) | ||
| In vivo | 30% PEG400/0.5% Tween80/5% propylene glycol, | 30 mg/mL | |
| * <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. | |||
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Preparing Stock Solutions
| Stock Solution (1ml DMSO) | 1mM | 10mM | 20mM | 30mM |
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| Mass(mg) | 0.56364 | 5.6364 | 11.2728 | 16.9092 |
