BI-847325

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.

BI-847325 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  BI-847325 is a selective dual MEK/Aurora kinase inhibitor with IC₅₀ values of 3, 25, 15, 25, and 4 nM for X. laevis Aurora B, human Aurora A and Aurora C, and human MEK1 and MEK2, respectively. It can inhibit the growth and survival of both treatment-naive and drug-resistant melanoma cell lines, decreasing the expression of MEK and Mcl-1 while increasing the expression of pro-apoptotic protein Bim. At 70 mg/kg, BI-847325 induces apoptosis in treatment-naive and drug-resistant xenografted melanoma in vivo.

• Verwenden

  BI-847325 is a novel ATP-competitive MEK and Aurora kinase inhibitor. It can inhibit the growth of BRAF resistant melanoma cells through suppression of Mcl-1 and MEK expression in human melanoma cell lines and mouse xenograft model. The efficacy of BI-847325 was studied in patients with refractory solid tumors.

• Einzelnachweise

  [1]. sini p, gürtler u, zahn sk, et al. pharmacological characterization of bi 847325, a dual inhibitor of mek and aurora kinases. cancer research, 2012, 72(8 supplement): 1919-1919.
  [2]. hideshima t, chauhan d, richardson p, et al. nf-κb as a therapeutic target in multiple myeloma. journal of biological chemistry, 2002, 277(19): 16639-16647.
  [3]. rommel c, clarke ba, zimmermann s, et al. differentiation stage-specific inhibition of the raf-mek-erk pathway by akt. science, 1999, 286(5445): 1738-1741..

BI-847325 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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