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Tocris Bioscience™ MS 39
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Catalog No. 73975
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73-975 5 mg
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Catalog No. 73-975 Supplier Tocris Bioscience™ Supplier No. 7397/5
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Description

Potent and selective VHL-recruiting Degrader (PROTAC™) of mutant EGFR

MS 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.

Specifications

Chemical Name or Material (2 S,4 R)-1-(-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
Quantity 5 mg
Target Active Degraders
Molecular Formula C55H71ClFN9O7S
Purity 0.98
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