E8284

(E/Z)-Endoxifen Hydrochloride Hydrate

≥98% (HPLC)

• Sinonimo/i: (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
• Formula empirica (notazione di Hill): C₂₅H₂₇NO₂ · HCl · xH₂O
• Peso molecolare: 409.95 (anhydrous basis)
• Numero MDL: MFCD16875406
• Codice UNSPSC: 12352203
• ID PubChem: 329799077
• NACRES: NA.77

Proprietà

• Saggio: ≥98% (HPLC)
• Forma fisica: solid
• Condizioni di stoccaggio: desiccated
• Colore: white to beige
• Solubilità: DMSO: >10 mg/mL
• Temperatura di conservazione: 2-8°C
• Stringa SMILE: 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-;;; BISAMGUAXFFKDX-NDIQBZANSA-N

Descrizione

Applicazioni

(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

Azioni biochim/fisiol

(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.

(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.

Caratteristiche e vantaggi

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.

Informazioni sulla sicurezza

• Codice della classe di stoccaggio: 11 - Combustible Solids
• Classe di pericolosità dell'acqua (WGK): nwg
• Punto d’infiammabilità (°F): Not applicable
• Punto d’infiammabilità (°C): Not applicable