SML2368
(Z)-Endoxifen
≥98% (HPLC)
Sinônimo(s):
4-Hydroxy-N-desmethyl-tamoxifen, Endoxifen, Metabolite BX, N-Desmethyl-4-hydroxytamoxifen, Z-Endoxifen
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About This Item
Fórmula empírica (Notação de Hill):
C25H27NO2
Número CAS:
Peso molecular:
373.49
Número MDL:
Código UNSPSC:
12352200
NACRES:
NA.77
Produtos recomendados
Ensaio
≥98% (HPLC)
forma
powder
cor
white to beige
solubilidade
DMSO: 2 mg/mL, clear
temperatura de armazenamento
2-8°C
Aplicação
(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.
Ações bioquímicas/fisiológicas
(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.
Palavra indicadora
Danger
Frases de perigo
Declarações de precaução
Classificações de perigo
Aquatic Acute 1 - Aquatic Chronic 1 - Carc. 1A - Repr. 1B
Código de classe de armazenamento
6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
Classe de risco de água (WGK)
WGK 3
Ponto de fulgor (°F)
Not applicable
Ponto de fulgor (°C)
Not applicable
Certificados de análise (COA)
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Paul Chen et al.
Cellular & molecular biology letters, 23, 3-3 (2018-01-09)
Endoxifen, an active metabolite of tamoxifen, has been shown to be an effective anti-estrogenic agent in estrogen receptor-positive breast cancer patients. In melanoma, estrogen receptor expression is shown to be associated with disease progression. However, the therapeutic benefit of endoxifen
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
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
Shagufta et al.
European journal of medicinal chemistry, 143, 515-531 (2017-12-06)
Tamoxifen (ICI 46 474), trans-1-(4-β-dimethylaminoethoxyphenyl)-1,2-diphenylbut-1-ene, is the most commonly used drug for the treatment of estrogen receptor positive breast cancer and has been saving lives worldwide for the past four decades. Tamoxifen is considered a pioneering drug due to its ubiquitous
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
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