Tocris Bioscience™ MS 39

Product Code. 18756556

Brand: Tocris Bioscience™ 7397/5

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