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Tocris Bioscience™ MS 154
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Catalog No. 73955
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Catalog No. Quantity
73-955 5 mg
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Catalog No. 73-955 Supplier Tocris Bioscience™ Supplier No. 7395/5
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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
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