MS 154

Name: MS 154
Brand: Tocris Bioscience
SKU: 7395

Tocris Bioscience, part of Bio-Techne | Catalog # 7395

COA / SDS

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

Key Product Details

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)
Molecular Weight:	901.43

View Full Technical Details for MS 154

Technical Data
Citations

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; 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.

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 for MS 154

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
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.

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