1032008-71-1|Endoxifen mesylate|4-[(Z)-1-[4-[2-(Methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol mesylate|-范德生物科技公司

Endoxifen mesylate

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names：
4-[(Z)-1-[4-[2-(Methylamino)ethoxy]phenyl]-2-phenylbut-1-enyl]phenol mesylate
CAS号：
1032008-71-1
MDL Number：
MF(分子式)： C26H31NO5S MW(分子量)： 469.596
EINECS: Reaxys Number:
Pubchem ID: Brand:BIOFOUNT

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中文别名	Endoxifen mesylate
英文别名	Endoxifen HCl; Endoxifen hydrochloride; Z-Endoxifen HCl; 4-Hydroxy-N-desmethyltamoxifen; N-Desmethyl-4-hydroxytamoxifen;
CAS号	1032008-71-1
Inchi	InChI=1S/C25H27NO2.CH4O3S/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;1-5(2,3)4/h4-16,26-27H,3,17-18H2,1-2H3;1H3,(H,2,3,4)/b25-24-;
InchiKey	NZSNFFJPXQBVFG-BJFQDICYSA-N
分子式 Formula	C26H31NO5S
分子量 Molecular Weight	469.596
溶解度Solubility
性状	Solid powder
储藏条件 Storage conditions	Dry, dark and store at 0-4℃ for short term (days to weeks) or -20℃ for long term (Store correctly 2-3years).

产品说明	Endoxifen mesylate(CAS:1032008-71-1 ):仅限应用于工业或者科学研究过程中非医疗目的，不应用于人类或动物的临床诊断以及治过程疗，该产品非药用，非食用。
Introduction	Endoxifen, also known as N-desmethyl-4-hydroxytamoxifen, is a chemical that is under development for estrogen receptor-positive breast cancer. It is also being evaluated as an antipsychotic for treatment of mania and other psychotic disorders. Endoxifen is a nonsteroidal selective estrogen receptor modulator (SERM) of the triphenylethylene group. It is an active metabolite of tamoxifen and has been found to be effective in patients that have failed previous hormonal therapies (tamoxifen, aromatase inhibitors, and fulvestrant). The prodrug tamoxifen is metabolized by the CYP2D6 enzyme to produce afimoxifene (4-hydroxytamoxifen) and endoxifen.
Application1
Application2
Application3

警示图
危险性	Warning
危险性警示
安全声明
安全防护
备注

[1]Barginear MF, Jaremko M, Peter I, Yu C, Kasai Y, Kemeny M, Raptis G, Desnick RJ. Increasing tamoxifen dose in breast cancer patients based on CYP2D6 genotypes and endoxifen levels: effect on active metabolite isomers and the antiestrogenic activity score. Clin Pharmacol Ther. 2011 Oct;90(4):605-1[1]doi: 10.1038/clpt.2011.153. Epub 2011 Sep 7. PubMed PMID: 21900890.

[2]Lin FI, Gonzalez EM, Kummar S, Do K, Shih J, Adler S, Kurdziel KA, Ton A, Turkbey B, Jacobs PM, Bhattacharyya S, Chen AP, Collins JM, Doroshow JH, Choyke PL, Lindenberg ML. Utility of (18)F-fluoroestradiol ((18)F-FES) PET/CT imaging as a pharmacodynamic marker in patients with refractory estrogen receptor-positive solid tumors receiving Z-endoxifen therapy. Eur J Nucl Med Mol Imaging. 2017 Mar;44(3):500-508. doi: 10.1007/s00259-016-3561-8. Epub 2016 Nov 21. PubMed PMID: 27872957.

[3] de Krou S, Rosing H, Nuijen B, Schellens JH, Beijnen JH. Fast and Adequate Liquid Chromatography-Tandem Mass Spectrometric Determination of Z-endoxifen Serum Levels for Therapeutic Drug Monitoring. Ther Drug Monit. 2017 Apr;39(2):132-137. doi: 10.1097/FTD.0000000000000372. PubMed PMID: 28045782.

[4] Reid JM, Goetz MP, Buhrow SA, Walden C, Safgren SL, Kuffel MJ, Reinicke KE, Suman V, Haluska P, Hou X, Ames MM. Pharmacokinetics of endoxifen and tamoxifen in female mice: implications for comparative in vivo activity studies. Cancer Chemother Pharmacol. 2014 Dec;74(6):1271-8. doi: 10.1007/s00280-014-2605-7. Epub 2014 Oct 16. PubMed PMID: 25318936; PubMed Central PMCID: PMC4343319.

[5] Ding S, Bierbach U. Linker design for the modular assembly of multifunctional and targeted platinum(ii)-containing anticancer agents. Dalton Trans. 2016 Aug 16;45(33):13104-13. doi: 10.1039/c6dt01399f. PubMed PMID: 27251881; PubMed Central PMCID: PMC4987242.

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