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MS 154

Cat. No. 7395 Submit a Review Datasheet / COA / SDS
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Description: Potent and selective cereblon-recruiting Degrader (PROTAC®) of mutant EGFR
Chemical Name: 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
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)
Biological Activity Technical Data Solubility Calculators Datasheets References

Biological Activity for MS 154

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) 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.

Technical Data for MS 154

M. Wt 901.43
Formula C46H54ClFN8O8
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2550393-21-8
PubChem ID 145996534
InChI Key ALKKWBPMCDDKKA-UHFFFAOYSA-N
Smiles COC1=CC2=C(C(NC3=CC(Cl)=C(C=C3)F)=NC=N2)C=C1OCCCN4CCN(CC4)CCC(NCCCCCCCCOC5=C6C(N(C(C6=CC=C5)=O)C7CCC(NC7=O)=O)=O)=O

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.

Solubility Data for MS 154

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 90.14 100

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 will affect the solvent volumes required to prepare stock solutions.

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

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References for MS 154

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

Cheng et al (2020) Discovery of potent and selective epidermal growth factor receptor (EGFR) bifunctional small-molecule degraders. J.Med.Chem. 63 1216 PMID: 31895569

If you know of a relevant reference for MS 154, please let us know.

View Related Products by Target

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Citations for MS 154

Citations are publications that use Tocris products.

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Literature in this Area

Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!

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TPD and Induced Proximity Research Product Guide

TPD and Induced Proximity Research Product Guide

This brochure highlights the tools and services available from Bio-Techne to support your Targeted Protein Degradation and Induced Proximity research, including:

  • Active Degraders
  • TAG Degradation Platform
  • Degrader Building Blocks
  • Assays for Protein Degradation
  • Induced Proximity Tools
Targeted Protein Degradation Poster

Targeted Protein Degradation Poster

Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia