SML2368

(Z)-Endoxifen

≥98% (HPLC)

• Synonyme(s) : 4-Hydroxy-N-desmethyl-tamoxifen, Endoxifen, Metabolite BX, N-Desmethyl-4-hydroxytamoxifen, Z-Endoxifen
• Formule empirique (notation de Hill) : C₂₅H₂₇NO₂
• CAS Number: 112093-28-4
• Poids moléculaire : 373.49
• Numéro MDL: MFCD09840374
• Code UNSPSC : 12352200
• Nomenclature NACRES : NA.77

Propriétés

• Essai: ≥98% (HPLC)
• Forme: powder
• Couleur: white to beige
• Solubilité: DMSO: 2 mg/mL, clear
• Température de stockage: 2-8°C
• Chaîne SMILES: 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-
• Clé InChI: MHJBZVSGOZTKRH-IZHYLOQSSA-N

Description

Application

(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.

Actions biochimiques/physiologiques

(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.

Informations sur la sécurité

• Pictogrammes: GHS08,GHS09
• Mention d'avertissement: Danger
• Mentions de danger: H350,H360,H410
• Conseils de prudence: P202 - P273 - P280 - P308 + P313 - P391 - P405
• Classification des risques: Aquatic Acute 1 - Aquatic Chronic 1 - Carc. 1A - Repr. 1B
• Code de la classe de stockage: 6.1C - Combustible acute toxic Cat.3 / toxic compounds or compounds which causing chronic effects
• Classe de danger pour l'eau (WGK): WGK 3
• Point d'éclair (°F): Not applicable
• Point d'éclair (°C): Not applicable