Chemical Name: N-(3-Fluoro-4-((7-(3-(3-(3-(((S)-1-((2S,4R)-4-hydroxy-2-((4-(4-methylthiazol-5-yl)benzyl)carbamoyl)pyrrolidin-1-yl)-3,3-dimethyl-1-oxobutan-2-yl)amino)-3-oxopropoxy)propoxy)propoxy)-6-methoxyquinolin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
Biological ActivitySJF 8240 is a c-MET PROTAC® Degrader. Comprises MET inhibitor foretinib joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Degrades c-MET within 6 hours in vitro. Inhibits agonist-driven AKT phosphorylation and GTL16 cell proliferation (IC50 = 66.7 nM). Also degrades exon-14-deleted c-MET in Hs746T cells.
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
The technical data provided above is for guidance only.
For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
The advantages of targeted protein degradation over inhibition: an RTK case study.
Burslem et al.
Cell Chem.Biol., 2018;25:67
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