3-{5-(4-bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid

3-{5-(4-bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid Chemische Eigenschaften,Einsatz,Produktion Methoden

• Beschreibung

  Poloppin is a modulator of protein-protein interactions of the mitotic polo-like kinases. It acts by targeting mutant KRAS, working synergistically with Crizotinib, an inhibitor of the c-MET receptor, against mutant KRAS-expressing cancer cells.

• Verwenden

  Poloppin is a potent, cell penetrant inhibitor of the mitotic Polo-like kinase (PLK) (IC50=26.9?μM) and prevents the protein-protein interaction via the Polo-box domain (PBD) (Kd= 29.5?μM). Poloppin selectively kills cells expressing mutant KRAS, enhancing death in mitosis.?Poloppin is used for the study of KRAS-mutant cancers as single agents, or in combination with c-MET inhibitors[1].

• Einzelnachweise

  [1] Ana J Narvaez, et al. Modulating Protein-Protein Interactions of the Mitotic Polo-like Kinases to Target Mutant KRAS. Cell Chem Biol. 2017 Aug 17;24(8):1017-1028.e7. DOI:10.1016/j.chembiol.2017.07.009

3-{5-(4-bromophenyl)-1-[2-(trifluoromethyl)phenyl]-1H-pyrrol-2-yl}propanoic acid Anbieter Lieferant Produzent Hersteller Vertrieb Händler.

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