SJF 1528
Tocris Bioscience, part of Bio-Techne | Catalog # 7262
Potent EGFR PROTAC® Degrader; also degrades HER2
Key Product Details
Description
Potent EGFR PROTAC® Degrader; also degrades HER2
Product Description
SJF 1528 is a potent EGFR PROTAC® Degrader (DC50 values are 39.2 nM for wild-type EGFR in OVCAR8 cells and 736 nM for Exon20Ins mutated EGFR in HeLa cells). Also degrades HER2. SJF 1528 comprises the EGFR inhibitor Lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Inhibits proliferation of HER2-driven breast cancer cell lines (IC50 = 102 nM for SKBr3 cells).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.
Product Specifications
Molecular Weight
1030.61
Formula
C55H57ClFN7O8S
Storage
Store at -20°C
Purity
≥98% (HPLC)
Chemical Name
(2S,4R)-1-((S)-2-(2-(2-(2-(4-(4-((3-Chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-
yl)phenoxy)ethoxy)ethoxy)acetamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
CAS Number
2230821-38-0
PubChem ID
135157151
InChI Key
ZSCOIFSUFMYZEZ-YSWDPXALSA-N
SMILES
CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCOCCOC4=CC=C(C5=CC6=C(N=CN=C6NC7=CC(Cl)=C(C=C7)OCC8=CC(F)=CC=C8)C=C5)C=C4)=O)=O)O)=O)SC=N1
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 | 103.06 | 100 |
Preparing Stock Solutions
for SJF 1528
The following data is based on the product molecular weight 1030.61
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 | 0.97 mL | 4.85 mL | 9.70 mL |
| 5 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 10 mM | 0.10 mL | 0.49 mL | 0.97 mL |
| 50 mM | 0.02 mL | 0.10 mL | 0.19 mL |
Calculators
Molarity Calculator
Dilution Calculator
Reconstitution Calculator
Background References
References are publications that support the biological activity of the product.
- Burslem The advantages of targeted protein degradation over inhibition: An RTK case study. Cell Chem.Biol. 2018 PMID: 29129716
Product Specific Notices for SJF 1528
For research use only
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