Chemical Name: (2S,4R)-1-((S)-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Biological ActivityMS 39 is a potent, high affinity and selective Degrader (PROTAC®) of mutant epidermal growth factor receptor (EGFR), comprising gefitinib (Iressa, Cat. No. 3000) conjugated via a linker to a VHL ligand. MS 39 potently induces degradation of mutant EGFR (DC50 values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cells in vitro, and is bioavailable in mice following ip administration.
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.
Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders.
Cheng et al.
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