Formulation: A solid
Formal Name: (2S,4R)-4-hydroxy-1-((S)-2-(2-(4-(3-methoxy-4-((4-((2-(methylcarbamoyl)phenyl)amino)-5-(trifluoromethyl)pyridin-2-yl)amino)phenyl)piperazin-1-yl)acetamido)-3,3-dimethylbutanoyl)-N-((S)-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide
Purity: ≥98%
Formula Markup: C50H59F3N10O6S
Formula Weight: 985,1
Shelf life (days): 1460
CAS Number: 2743427-26-9
Notes: GSK215 is a proteolysis-targeting chimera (PROTAC) composed of the focal adhesion kinase (FAK) inhibitor PND1186 (Item No. 17668) linked to the von-Hippel Lindau (VHL) E3 ligase ligand VHL-021.{66829} It binds to the FAK kinase domain (IC50 = 15.8 nM) and induces FAK degradation in A549 lung cancer cells with a 50% degradation concentration (DC50) of 1.3 nM. GSK215 (100 nM) inhibits A549 cell migration and invasion. In vivo, GSK215 (8 mg/kg) reduces hepatic FAK levels in mice.
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