MS 39

Name: MS 39
Brand: Tocris Bioscience
SKU: 7397

Tocris Bioscience, part of Bio-Techne | Catalog # 7397

COA / SDS

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

Key Product Details

Description:	Potent and selective VHL-recruiting Degrader (PROTAC^®) of mutant EGFR
Chemical Name:	(2S,4R)-1-((S)-2-(11-(4-(3-((4-((3-Chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)propyl)piperazin-1-yl)-11-oxoundecanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity:	≥98% (HPLC)
Molecular Weight:	1056.74

View Full Technical Details for MS 39

Technical Data
Citations

Biological Activity for MS 39

MS 39 is a potent, high affinity and selective Degrader (PROTAC^®) of mutant epidermal growth factor receptor (EGFR), comprising gefitinib (Iressa, Cat. No. 3000) conjugated via a linker to a VHL ligand. MS 39 potently induces degradation of mutant EGFR (DC₅₀ values are 5 nM and 3.3 nM in HCC827 (exon 19 del) and H3255 (L858R mutation) lung cancer cell lines, respectively), but exhibits no significant effect in cell lines bearing wild-type EGFR at concentrations up to 10 μM. MS 39 inhibits proliferation of H3255 lung cancer cells in vitro, and is bioavailable in mice following ip administration.

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 39

M. Wt	1056.74
Formula	C₅₅H₇₁ClFN₉O₇S
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	2675490-92-1
PubChem ID	145996533
InChi Key	HLFLODKZIGYHNR-LTEFSYCBSA-N
Smiles	COC1=CC2=NC=NC(NC3=CC(Cl)=C(C=C3)F)=C2C=C1OCCCN4CCN(CC4)C(CCCCCCCCCC(N[C@@H](C(C)(C)C)C(N5C[C@@H](C[C@H]5C(NCC6=CC=C(C=C6)C7=C(N=CS7)C)=O)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 39

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	105.67	100

Preparing Stock Solutions for MS 39

The following data is based on the product molecular weight 1056.74.

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	0.95 mL	4.73 mL	9.46 mL
5 mM	0.19 mL	0.95 mL	1.89 mL
10 mM	0.09 mL	0.47 mL	0.95 mL
50 mM	0.02 mL	0.09 mL	0.19 mL

Molarity Calculator

Calculate the mass, volume, or concentration required for a solution.

Mass

Concentration

Volume

M. Wt*

g/mol

*When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and CoA (available online).

Dilution Calculator

Calculate the dilution required to prepare a stock solution.

Concentration 1 (C1)

Volume 1 (V1)

Concentration 2 (C2)

Volume 2 (V2)

Reconstitution Calculator

The reconstitution calculator allows you to quickly calculate the volume of a reagent to reconstitute your vial. Simply enter the mass of reagent and the target concentration and the calculator will determine the rest.

Volume (to add to vial)

Mass (in vial)

Desired Reconstitution Concentration

References for MS 39

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