Identification | Back Directory | [Name]
Foretinib-Based PROTAC 7 | [CAS]
2230821-68-6 | [Synonyms]
Foretinib-Based PROTAC 7 1-N'-[3-fluoro-4-[7-[3-[3-[3-[[(2R)-1-[(2R,4S)-4-hydroxy-2-[[4-(4-methyl-1,3-thiazol-5-yl)phenyl]methylcarbamoyl]pyrrolidin-1-yl]-3,3-dimethyl-1-oxobutan-2-yl]amino]-3-oxopropoxy]propoxy]propoxy]-6-methoxyquinolin-4-yl]oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide | [Molecular Formula]
C58H65F2N7O11S | [MOL File]
2230821-68-6.mol | [Molecular Weight]
1106.25 |
Chemical Properties | Back Directory | [Boiling point ]
1226.5±65.0 °C(Predicted) | [density ]
1.341±0.06 g/cm3(Predicted) | [storage temp. ]
Store at -20°C | [solubility ]
DMSO|55.31|50| | [form ]
Solid | [pka]
13.14±0.70(Predicted) | [color ]
White to light yellow |
Hazard Information | Back Directory | [Description]
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. | [Uses]
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]. | [storage]
Store at -20°C | [References]
[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 |
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