2230821-68-6

SJF-8240 is a c-MET degrader. It comprises MET inhibitor foretinib joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. SJF-8240 degrades c-MET within 6 hours in vitro and inhibits agonist-driven AKT phosphorylation and GTL16 cell proliferation. It also degrades exon-14-deleted c-MET in Hs746T cells.

SJF-8240 (PROTAC 7) is a proteolysis targeting chimera (PROTAC) degrader. SJF-8240 induces polyubiquitination of c-Met and inhibits the proliferation of GTL16 cells (IC50=66.7 nM)[1].

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[1] Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3. DOI:10.1016/j.chembiol.2017.09.009