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Merck
CN

SML2368

Sigma-Aldrich

(Z)-Endoxifen

≥98% (HPLC), selective estrogen receptor modulator, powder

别名:

4-Hydroxy-N-desmethyl-tamoxifen, Endoxifen, Metabolite BX, N-Desmethyl-4-hydroxytamoxifen, Z-Endoxifen

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关于此项目

经验公式(希尔记法):
C25H27NO2
化学文摘社编号:
分子量:
373.49
MDL编号:
UNSPSC代码:
12352200
NACRES:
NA.77
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产品名称

(Z)-Endoxifen, ≥98% (HPLC)

方案

≥98% (HPLC)

表单

powder

颜色

white to beige

溶解性

DMSO: 2 mg/mL, clear

储存温度

2-8°C

SMILES字符串

N(CCOc1ccc(cc1)\C(=C(\CC)/c3ccccc3)\c2ccc(cc2)O)C

InChI

1S/C25H27NO2/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/b25-24-

InChI key

MHJBZVSGOZTKRH-IZHYLOQSSA-N

应用

(Z)-Endoxifen has been used to demonstrate the lack of contribution of subventricular zone and leptomeningeal cells in a study determining the generation of neuroblasts from astrocytes.

生化/生理作用

(Z)-Endoxifen (endoxifen) is an active tamoxifen metabolite generated via actions of cytochrome P450 (CYP) enzymes CYP3A4/5 and CYP2D6. Endoxifen is more potent than tamoxifen as a selective estrogen receptor modulator (SERM) both in vitro and in vivo with good pharmacokinetics and oral availability (∼80% MCF-7 tumor growth inhibition with 4-8 mg/kg/day endoxifen or 20 mg/kg/day tamoxifen in mice via p.o.). Endoxifen also exhibits 4-fold higher PKC inhibitory potency than tamoxifen and can overcome tamoxifen resistance due to cytochrome CYP2D6 polymorphism.
Orally available, active tamoxifen metabolite with higher estrogen receptor modulator (SERM) activity and anticancer efficacy both in vitro and in vivo.

象形图

Health hazardEnvironment

警示用语:

Danger

危险声明

危险分类

Aquatic Acute 1 - Aquatic Chronic 1 - Carc. 1A - Repr. 1B

储存分类代码

6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


历史批次信息供参考:

分析证书(COA)

Lot/Batch Number

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Vered Stearns et al.
Journal of the National Cancer Institute, 95(23), 1758-1764 (2003-12-05)
Tamoxifen, a selective estrogen receptor modulator (SERM), is converted to 4-hydroxy-tamoxifen and other active metabolites by cytochrome P450 (CYP) enzymes. Selective serotonin reuptake inhibitors (SSRIs), which are often prescribed to alleviate tamoxifen-associated hot flashes, can inhibit CYPs. In a prospective
Phyllis Elkins et al.
Journal of pharmaceutical and biomedical analysis, 88, 174-179 (2013-09-24)
(Z)-Endoxifen (4-hydroxy-N-desmethyltamoxifen), an active metabolite generated via actions of CYP3A4/5 and CYP2D6, is a more potent selective estrogen receptor modulator (SERM) than tamoxifen. In the MCF-7 human mammary tumor xenograft model with female athymic mice, (Z)-endoxifen, at an oral dose
Janina Johänning et al.
Archives of toxicology, 92(3), 1099-1112 (2017-12-30)
Tamoxifen, a standard therapy for breast cancer, is metabolized to compounds with anti-estrogenic as well as estrogen-like action at the estrogen receptor. Little is known about the formation of estrogen-like metabolites and their biological impact. Thus, we characterized the estrogen-like
Matthew P Goetz et al.
Journal of clinical oncology : official journal of the American Society of Clinical Oncology, 35(30), 3391-3400 (2017-08-31)
Purpose Endoxifen is a tamoxifen metabolite with potent antiestrogenic activity. Patients and Methods We performed a phase I study of oral Z-endoxifen to determine its toxicities, maximum tolerated dose (MTD), pharmacokinetics, and clinical activity. Eligibility included endocrine-refractory, estrogen receptor-positive metastatic
E A Lien et al.
Cancer research, 48(8), 2304-2308 (1988-04-15)
The occurrence of tamoxifen metabolites in bile was investigated in a 57-year-old female patient receiving chronic treatment with tamoxifen. In bile treated with beta-glucuronidase, two major peaks were detected using a chromatographic system developed for the quantitation of tamoxifen metabolites

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