Endoxifen HCl

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Endoxifen HCl

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:	1032008-74-4
规格:	≥98%

包装与价格：

包装	价格(元)
5mg	电议
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议

产品介绍

Endoxifen HCl (Z-Endoxifen; N-Desmethyl-4-hydroxytamoxifen), the hydrochloride salt of endoxifen which is an active metabolite of Tamoxifen, is a potent and selective estrogen receptor antagonist/SERM with potential anticancer activity. It has been found to be effective in patients that have failed previous hormonal therapies. 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.

理化性质和储存条件

Molecular Weight (MW)	409.95
Formula	C25H28ClNO2
CAS No.	1032008-74-4
Storage	-20℃ for 3 years in powder form
Storage	-80℃ for 2 years in solvent
Solubility (In vitro)	DMSO: 74 mg/mL (180.5 mM)
	Water: <1 mg/mL
	Ethanol: 74 mg/mL (180.5 mM)
Other info	Chemical Name: (Z)-4-(1-(4-(2-(methylamino)ethoxy)phenyl)-2-phenylbut-1-en-1-yl)phenol hydrochloride InChi Key: RPFIMPDXTABYCN-BJFQDICYSA-N InChi Code: InChI=1S/C25H27NO2.ClH/c1-3-24(19-7-5-4-6-8-19)25(20-9-13-22(27)14-10-20)21-11-15-23(16-12-21)28-18-17-26-2;/h4-16,26-27H,3,17-18H2,1-2H3;1H/b25-24-; SMILES Code: OC1=CC=C(/C(C2=CC=C(OCCNC)C=C2)=C(C3=CC=CC=C3)\CC)C=C1.[H]Cl
Synonyms	Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; Endoxifen hydrochloride; N-Desmethyl-4-hydroxytamoxifen

实验参考方法

In Vitro	In vitro activity: 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 Cell Assay: 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.
In Vivo	In vivo, Endoxifen (8 mg/kg, ) inhibits growth of MCF-7 human mammary tumor xenografts in mice, showing more potency than Tamoxifen.
Animal model	Mice bearing MCF-7 human mammary tumor xenografts
Formulation & Dosage	Dissolved in water; 8 mg/kg; Oral gavage
References	Cancer Chemother Pharmacol. 2005 May;55(5):471-8; Breast Cancer Res Treat. 2010 Jul;122(2):579-84.