MS 154

Key Product Details

Product Description

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.

Licensing Information

Sold under license from Icahn School of Medicine at Mount Sinai.

Product Specifications for MS 154

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Solubility

Preparing Stock Solutions for MS 154

The following data is based on the product molecular weight 901.43.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

1 Recalculate

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.11 mL	5.55 mL	11.09 mL
5 mM	0.22 mL	1.11 mL	2.22 mL
10 mM	0.11 mL	0.55 mL	1.11 mL
50 mM	0.02 mL	0.11 mL	0.22 mL

Calculators

Background References

References are publications that support the biological activity of the product.

• Cheng Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders. J.Med.Chem. 2020 PMID: 31895569

Product Documents for MS 154