Endoxifen HCl

製品コードS7839 バッチS783902

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
* <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

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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：

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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