N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

  H315：Verursacht Hautreizungen.

  H319：Verursacht schwere Augenreizung.

  H335：Kann die Atemwege reizen.

• Sicherheit

  P261：Einatmen von Staub vermeiden.

  P305+P351+P338：BEI KONTAKT MIT DEN AUGEN: Einige Minuten lang behutsam mit Wasser spülen. Eventuell vorhandene Kontaktlinsen nach Möglichkeit entfernen. Weiter spülen.

N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  EPZ020411 hydrochloride is a potent and selective small molecule inhibitor of PRMT6 with IC50 of 10 nM.

• in vitro

  EPZ020411 hydrochloride dose-dependently reduced H3R2 methylation in human melanoma A375 cells overexpressing PRMT6 (IC50=0.637±0.241 μM). In biochemical assays, the selectivity of EPZ020411 to PRMT6/8/1 was more than 100-fold higher than that of other histone methyltransferases (including 4 arginine methyltransferases PRMT3, PRMT4, PRMT5, PRMT7). In the parallel artificial membrane permeation test, EPZ020411 has poor permeability.

• in vivo

  EPZ020411 hydrochloride has good bioavailability in rats by subcutaneous injection and is a suitable compound for in vivo studies. After a single intravenous injection of 1 mg/kg EPZ020411 hydrochloride into male Sprague-Dawley rats, its in vivo clearance (CL) was 19.7 ± 1.0 mL/min/kg and its volume of distribution at steady state (Vss) was 11.1 ± 1.6 L/kg, the average half-life was 8.54±1.43 h. Subcutaneous injection of 5 mg/kg has good bioavailability of 65.6 ± 4.3%, and the free concentration of EPZ020411 in the blood is higher than the biochemical IC50 value of PRMT6 for more than 12 hours.

• target

  < td style="border-bottom: 1px dotted #ccc;padding: 5px;"> PRMT8
  (Cell-free assay)

  Target	Value
  PRMT6 (Cell-free assay)	10 nM
  PRMT1 (Cell-free assay)	119 nM
  223 nM

N1,N2-Dimethyl-N1-[[3-[4-[[trans-3-[2-(tetrahydro-2H-pyran-4-yl)ethoxy]cyclobutyl]oxy]phenyl]-1H-pyrazol-4-yl]methyl]-1,2-ethanediamine hydrochloride Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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