TAS-116

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.

TAS-116 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  TAS-116 is a novel small molecule inhibitor of HSP90 with Ki values of 34.7 nmol/L and 21.3 nmol/L for HSP90α and HSP90β, respectively. It does not inhibit other ATPases such as HSP70 (IC50 >200 μmol/L).

• in vitro

  TAS-116 is a selective inhibitor of HSP90α and HSP90β in the cytoplasm, but has no inhibitory effect on endoplasmic reticulum GRP94 or mitochondrial TRAP1. Treatment of HCT116 cells with 0.3 μM of TAS-1116 for 8 hours resulted in a decrease in DDR1 levels and induction of HSP70.

• in vivo

  In a mouse model with human xenograft tumors, oral administration of TAS-116 induced tumor shrinkage accompanied by depletion of HSP90. In a rat model, TAS-116 was more distributed in subcutaneously xenografted NCI-H1975 non-small cell lung cancer tumors than in the retina. TAS-116 was also active in orthotopically transplanted NCI-H1975 lung tumors.

• target

  Target	Value
  HSP90β (Cell-free assay)	21.3 nM(Ki)
  HSP90α (Cell-free assay )	34.7 nM(Ki)

TAS-116 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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