受注:045-509-1970 |
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Synonyms | N/A | Storage (From the date of receipt) |
3 years -20°C powder 1 years -80°C in solvent |
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化学式 | C25H28ClNO2 |
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分子量 | 409.95 | CAS No. | 1032008-74-4 | ||||||||
Solubility (25°C)* | 体外 | DMSO | 74 mg/mL (180.5 mM) | ||||||||
Ethanol | 74 mg/mL (180.5 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. |
製品説明 | Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2. |
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in vitro | Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. [1] Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. [2] In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. [3] Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. [4] Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM. [5] |
in vivo | In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen. [3] |
細胞アッセイ | 細胞株 | MCF7 and Ishikawa cells |
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濃度 | 1000 nM | |
反応時間 | 8 days | |
実験の流れ | MCF7 and Ishikawa cells are grown in 10% triple charcoal-stripped serum-containing medium for 3 d. The cells are then plated at a density of 2,000 cells per well in 96-well tissue culture plates and treated as indicated every 48 h. Cell proliferation assays are conducted 8 days after the first treatment using a CellTiter-Glo Luminescent Cell Viability kit according to the manufacturer's protocol. | |
動物実験 | 動物モデル | Mice bearing MCF-7 human mammary tumor xenografts |
投薬量 | 8 mg/kg | |
投与方法 | p.o. |
Identification of the estrogen receptor beta as a possible new tamoxifen-sensitive target in diffuse large B-cell lymphoma [ Blood Cancer J, 2022, 12(3):36] | PubMed: 35256592 |
Fatty acid oxidation and autophagy promote endoxifen resistance and counter the effect of AKT inhibition in ER-positive breast cancer cells [ J Mol Cell Biol, 2021, mjab018] | PubMed: 33755174 |
Targeting Estrogen Receptor-Positive Breast Microtumors with Endoxifen-Conjugated, Hypoxia-Sensitive Polymersomes [ ACS Omega, 2021, 6(42):27654-27667] | PubMed: 34722965 |
The effect of oestrogen on mandibular condylar cartilage via hypoxia-inducible factor-2α during osteoarthritis development. [ Bone, 2020, 130:115123] | PubMed: 31678498 |
Estrogen-Related Hormones Induce Apoptosis by Stabilizing Schlafen-12 Protein Turnover. [ Mol Cell, 2019, 75(6):1103-1116.e9] | PubMed: 31420216 |
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。