MS 154

Biological Activity

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; D_max > 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) and EGFR antibody validated for Simple Western™ (automated Western) instruments and Western Blot also available: Catalog # AF231.

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

Technical Data

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.

Additional Information

Background References

1. Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders.
   Cheng et al.
   J.Med.Chem., 2020;63:1216

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