Tocris Bioscience™ MS 154

Description

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

MS 154 is a potent and selective cereblon-recruiting Degrader (PROTAC™) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon-binding moiety joined by a linker to gefitinib (Iressa, Cat. No. 3000). MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR-bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC-827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT-EGFR-bearing ovarian and lung cancer cells lines. Bioavailable in mice following ip administration.

Negative control (Cat. No. 7396) also available.

PROTAC™ is a registered trademark of Arvinas Operations, Inc., and is used under license.

Specifications

• Chemical Name or Material: 3-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-N-(8-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-4-yl)oxy)octyl)propanamide
• CAS: 2550393-21-8
• Quantity: 5 mg
• Target: Active Degraders
• Molecular Formula: C₄₆H₅₄ClFN₈O₈
• Purity: 0.98