Endoxifen HCl

製品コードS7839 バッチS783902

印刷

化学情報

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

81 mg/mL (197.58 mM)

Ethanol

81 mg/mL (197.58 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.

* <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は、タモキシフェンの活性代謝物であり、強力で選択的なエストロゲン受容体拮抗薬です。第2相。
in vitro	Endoxifen shows anti-estrogenic effects, and decreases the E2-induced PR expression in MCF-7 cells. Endoxifen also blocks ER-alpha transcriptional activity and inhibits estrogen-induced breast cancer cell proliferation. In MCF7, HS 578T, and BT-549 cells, Endoxifen significantly inhibits cell proliferation. Endoxifen also exhibits four-fold higher inhibition on PKC activity compared to tamoxifen. Endoxifen inhibits the hERG current by preferentially interacting with the activated states of cloned hERG potassium channels with IC50 of 1.6 μM.
in vivo	In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen.

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/

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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。

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