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2230821-68-6

2230821-68-6 Structure

2230821-68-6 Structure
IdentificationBack 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 PropertiesBack 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 InformationBack 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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