Endoxifen HCl

製品コードS7839 バッチS783901

印刷

化学情報

Chemical Structure Synonyms N/A Storage
(From the date of receipt)		 3 years -20°C powder
1 years -80°C in solvent
化学式

C25H28ClNO2
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）
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution
5% DMSO 20% PEG 300 5%Tween80 70% water

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 2.500mg/ml (6.10mM) Taking the 1 mL working solution as an example, add 50 μL of 50 mg/ml clarified DMSO stock solution to 200 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify it; then continue adding Adjust the volume to 1 mL with 700 μL ddH2O. The mixed solution should be used immediately for optimal results. 
Clear solution
5% DMSO 95% corn oil

この製剤はselleckのラボで検証済みです。上記の溶解方法がご要望を満たさない場合、selleckの営業担当までお問い合わせ頂ければ、個別の試験を行います。

 0.300mg/ml (0.73mM) Taking the 1 mL working solution as an example, add 50 μL of 6 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results. 
* <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.

溶剤液（一定の濃度）を調合する

生物活性

製品説明 Endoxifen HCl, the active metabolite of Tamoxifen, ia a potent and selective estrogen receptor antagonist. Phase 2.
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]

プロトコル(参考用のみ)

細胞アッセイ 細胞株 MCF7 and Ishikawa cells
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.

参考

  • https://pubmed.ncbi.nlm.nih.gov/15685451/
  • https://pubmed.ncbi.nlm.nih.gov/19244106/
  • https://pubmed.ncbi.nlm.nih.gov/20052538/
  • https://pubmed.ncbi.nlm.nih.gov/20227879/
  • https://pubmed.ncbi.nlm.nih.gov/25680947/

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：

Antiviral Activity of Selective Estrogen Receptor Modulators against Severe Fever with Thrombocytopenia Syndrome Virus In Vitro and In Vivo [ Viruses, 2024, 16(8)1332] PubMed: 39205306
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。