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受注：045-509-1970 |
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化学情報
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Synonyms | ICI 46474, Istubal | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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| 化学式 | C26H29NO.C6H8O7 |
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| 分子量 | 563.64 | CAS No. | 54965-24-1 | ||||
| Solubility (25°C)* | 体外 | DMSO | 100 mg/mL (177.41 mM) | ||||
| Ethanol | 5 mg/mL (8.87 mM) | ||||||
| Water | Insoluble | ||||||
| 体内 （毎回新しく調製した物を用意してください） |
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* <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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溶剤液（一定の濃度）を調合する
生物活性
| 製品説明 | 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 Citrate displays antitumor effect due to its antiestrogenic activity (ER). Values for the apparent affinity of this compound 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 this chemical 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. It also directly induces programmed cell death. [1] This compound 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 this chemical on MCF-7 cell growth can be readily reversed by addition of estradiol to the culture medium. 2 and 6 μM of this agent reduces the proportion of cells in S phase and increases the number of cells in G1. At 10 μM, it causes cell death within 48 hr. [2] This compound inhibits MCF-7 growth with IC50 of ~10 nM after 10 days treatment. It inhibits plasminogen activator activity of MCF-7, and suppresses estradiol-stimulation of plasminogen activator activity. This chemical also evokes minimal increases in cellular progesterone receptor levels. [3] It 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 Citrate 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. This compound 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] It has not only antiestrogenic but also estrogenic properties depending on the species, tissue, and gene. This chemical displays favorable effects on bone and serum lipid concentrations and stimulation endometrium. [1] |
プロトコル(参考用のみ)
| キナーゼアッセイ | Competitive binding assays | |
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| 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 this compound 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%. | ||
| 細胞アッセイ | 細胞株 | Human breast cancer cells MCF-7 |
| 濃度 | ~1 μM | |
| 反応時間 | 10 days | |
| 実験の流れ | 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 this compound. At the end of incubation, cell numbers are counted. |
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| 動物実験 | 動物モデル | Human breast carcinoma xenografts MCF-7 |
| 投薬量 | 2 cm Tamoxifen capsules | |
| 投与方法 | Subcutaneous implantation | |
参考
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カスタマーフィードバック
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, , University of North Texas Health Science Center, 2014.
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：
| Minute amounts of helicase-deficient truncated RECQL4 are sufficient for DNA replication [ bioRxiv, 2025, 2025.07.21.666025] | PubMed: 40777487 |
| Mcam stabilizes luminal progenitor breast cancer phenotypes via Ck2 control and Src/Akt/Stat3 attenuation [ bioRxiv, 2024, 2023.05.10.540211] | PubMed: 38562809 |
| The phenotype of the most common human ADAR1p150 Zα mutation P193A in mice is partially penetrant [ EMBO Rep, 2023, 24(5):e55835] | PubMed: 36975179 |
| Smoothened antagonist sonidegib affects the development of D. melanogaster larvae via suppression of epidermis formation [ Pestic Biochem Physiol, 2023, 194:105462] | PubMed: 37532307 |
| 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 |
長期の保管のために-20°Cの下で製品を保ってください。
人間や獣医の診断であるか治療的な使用のためにでない。
各々の製品のための特定の保管と取扱い情報は、製品データシートの上で示されます。大部分のSelleck製品は、推薦された状況の下で安定です。製品は、推薦された保管温度と異なる温度で、時々出荷されます。長期の保管のために必要とされてそれと異なる温度で、多くの製品は、短期もので安定です。品質を維持するが、夜通しの積荷のために最も経済的な貯蔵状況を用いてあなたの送料を保存する状況の下に、製品が出荷されることを、我々は確実とします。製品の受領と同時に、製品データシートの上で貯蔵推薦に従ってください。