MS 39

Tocris Bioscience | Catalog # 7397

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

Key Product Details

Description

Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
View all Active Degraders »

Product Description

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.

Product Specifications for MS 39

Molecular Weight

1056.74

Formula

C55H71ClFN9O7S

Storage

Store at -20°C

Purity

≥98% (HPLC)

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

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.

Solubility

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

Calculators

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Background References

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

Product Documents for MS 39

Certificate of Analysis

To download a Certificate of Analysis, please enter a lot or batch number in the search box below.

Product Specific Notices for MS 39

For research use only

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