S49076

Gefahreninformationscode (GHS)

• Bildanzeige (GHS)

  

• Alarmwort

  Warnung

• Gefahrenhinweise

  H302：Gesundheitsschädlich bei Verschlucken.

• Sicherheit

  P280：Schutzhandschuhe/Schutzkleidung/Augenschutz tragen.

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

S49076 Chemische Eigenschaften,Einsatz,Produktion Methoden

• Biologische Aktivität

  S49076 is a novel and potent inhibitor of Met (c-Met), AXL/MER and FGFR1/2/3 with IC50 below 20 nM.

• in vivo

  S49076 effectively inhibits the phosphorylation of MET, AXL and FGFRs in cells, and inhibits their downstream signaling pathways in vitro and in vivo. In cellular models, it inhibits MET and FGFR2-dependent gastric cancer cells, prevents MET-driven migration of lung cancer cells, and inhibits colony formation of liver cancer cells expressing FGFR1/2 and AXL. S49076 inhibits cell viability, motile, three-dimensional colony formation of cancer cells expressing MET, AXL or FGFRs.

• in vivo

  S49076 has significant antitumor activity in MET- and FGFR-dependent tumor grafts. It is highly distributed in tumors, with a half-life of approximately 7 hours in tumors and less than 2 hours in blood at a dose of 3.125 mg/kg. At doses above 6.25 mg/kg, more than 50% of MET phosphorylation was inhibited for 16 hours. S49076 was also active in a bevacizumab-resistant model, and in combination with bevacizumab, completely inhibited the growth of colon cancer xenografts.

• target

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

  Target	Value
  Met (Cell-free assay)	1 nM
  Mer (Cell-free assay)	2 nM
  7 nM
  FGFR3 (Cell-free assay)	15 nM
  FGFR2 (Cell-free assay)	17 nM

S49076 Upstream-Materialien And Downstream Produkte

S49076 Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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