E8284

(E/Z)-Endoxifen Hydrochloride Hydrate

≥98% (HPLC), Selective Estrogen response modifier (SERM), solid

• Synonyma: (E/Z)-Endoxifen hydrochloride hydrate, (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
• Empirický vzorec (Hillův zápis): C₂₅H₂₇NO₂ · HCl · xH₂O
• Molekulová hmotnost: 409.95 (anhydrous basis)
• UNSPSC Code: 12352203
• PubChem Substance ID: 329799077
• NACRES: NA.77
• MDL number: MFCD16875406
• Assay: ≥98% (HPLC)
• Form: solid
• Storage condition: desiccated

Vlastnosti

• Název produktu: (E/Z)-Endoxifen Hydrochloride Hydrate, ≥98% (HPLC)
• Quality Segment: 100
• assay: ≥98% (HPLC)
• form: solid
• storage condition: desiccated
• color: white to beige
• solubility: DMSO: >10 mg/mL
• storage temp.: 2-8°C
• SMILES string: O.Cl.CC\C(c1ccccc1)=C(/c2ccc(O)cc2)c3ccc(OCCNC)cc3
• InChI: 1S/C25H27NO2.ClH.H2O/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;1H2/b25-24-;;
• InChI key: BISAMGUAXFFKDX-NDIQBZANSA-N

Popis

Application

(E/Z)-Endoxifen Hydrochloride Hydrate has been used:
as a selective estrogen receptor modulator (SERM) to study the role of miR-27a expression
to impregnate a biocompatible polymer in the subcutaneous space adjacent to the TA muscle of PDGFRαCreER;R26NG mice
to study its in vivo performance and properties for CreERT2 (mutant estrogen receptor) control

Biochem/physiol Actions

(E/Z)-endoxifen hydrochloride may be used in hormone therapy to fight breast cancer. Endoxifen is considered as an active metabolite of tamoxifen. Hence it is responsible for the tamoxifen activity in the human body.

(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.

Tamoxifen metabolite; Selective Estrogen response modifier (SERM) .

Features and Benefits

This compound is featured on the Nuclear Receptors (Steroids) page of the Handbook of Receptor Classification and Signal Transduction. To browse other handbook pages, click here.

Bezpečnostní informace

• Skladovací třída: 11 - Combustible Solids
• Co se děje?: nwg
• Bod vzplanutí (°F): Not applicable
• Bod vzplanutí (°C): Not applicable