(E/Z)-Endoxifen Hydrochloride Hydrate

• Catalog No.: E8284
• M. F.: C25H30ClNO3
• M. W.: 427.9636
• Purity: ≥98% (HPLC)
• Storage: desiccated

SYNONYMS

• IUPAC name: 4-(1-{4-[2-(methylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl)phenol hydrate hydrochloride
• IUPAC Traditional name: 4-(1-{4-[2-(methylamino)ethoxy]phenyl}-2-phenylbut-1-en-1-yl)phenol hydrate hydrochloride
• Synonyms: (E/Z)-4-Hydroxy-N-desmethyltamoxifen hydrochloride hydrate; (E/Z)-4-[1-[4-[2-(Methylamino)ethoxy]phenyl]-2-phenyl-1-buten-1-yl]-phenol hydrochloride hydrate (1:1 E/Z mixture); (E/Z)-4OHNDtam hydrochloride hydrate; (E/Z)-Endoxifen hydrochloride hydrate

DATABASE IDS

• MDL Number: MFCD16875406

PROPERTIES

• Empirical Formula (Hill Notation): C25H27NO2 · HCl · xH2O
• Purity: ≥98% (HPLC)
• Apperance: white to beige solid
• Solubility: DMSO: >10 mg/mL
• Storage Condition: desiccated
• Storage Temperature: 2-8°C
• German water hazard class: nwg

DETAILS

Description (English)

Biochem/physiol Actions
(E/Z)-Endoxifen hydrochloride ((E/Z)-4-Hydroxy-N-desmethyltamoxifen hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). It is equipotent to 4-hydroxytamoxifen with respect to estrogen receptor binding and inhibition of 17-estradiol (E2)-induced cell proliferation. It is primarily catalyzed by cytochrome P450 2D6 (CYP2D6). Mutations in CYP2D6 may prevent response to tamoxifen by preventing formation of endoxifen. The gene expression patterns of five genes have been validated to be differentially regulated by endoxifen and 4-OH-Tamoxifen. Endoxifen and 4-OH-Tam have similar effects on global gene expression patterns in MCF-7 cells and the majority of the affected genes are estrogen-regulated genes.

Description (简体中文)

Biochem/physiol Actions
(E/Z)-Endoxifen hydrochloride ((E/Z)-4-Hydroxy-N-desmethyltamoxifen hydrochloride) is a tamoxifen metabolite and potent Selective Estrogen Response Modifier (SERM). It is equipotent to 4-hydroxytamoxifen with respect to estrogen receptor binding and inhibition of 17-estradiol (E2)-induced cell proliferation. It is primarily catalyzed by cytochrome P450 2D6 (CYP2D6). Mutations in CYP2D6 may prevent response to tamoxifen by preventing formation of endoxifen. The gene expression patterns of five genes have been validated to be differentially regulated by endoxifen and 4-OH-Tamoxifen. Endoxifen and 4-OH-Tam have similar effects on global gene expression patterns in MCF-7 cells and the majority of the affected genes are estrogen-regulated genes.