MS 39
Tocris Bioscience, part of Bio-Techne | Catalog # 7397
Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
Key Product Details
Description
Potent and selective VHL-recruiting Degrader (PROTAC®) of mutant EGFR
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
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.
| 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
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
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 Specific Notices for MS 39
For research use only
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