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Submit ReviewSJF 1528
Description: Potent EGFR PROTAC®; also degrades HER2
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
Purity: ≥98% (HPLC)
Biological Activity for SJF 1528
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).
PROTAC® is a registered trademark of Arvinas Operations, Inc., and is used under license.
Technical Data for SJF 1528
| M. Wt | 1030.61 |
| Formula | C55H57ClFN7O8S |
| Storage | Store at -20°C |
| Purity | ≥98% (HPLC) |
| 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.
Tocris products are intended for laboratory research use only, unless stated otherwise.
Solubility Data for SJF 1528
| 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 will 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 | 9.7 mL |
| 5 mM | 0.19 mL | 0.97 mL | 1.94 mL |
| 10 mM | 0.1 mL | 0.49 mL | 0.97 mL |
| 50 mM | 0.02 mL | 0.1 mL | 0.19 mL |
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Product Datasheets for SJF 1528
References for SJF 1528
References are publications that support the biological activity of the product.
Burslem et al (2018) The advantages of targeted protein degradation over inhibition: An RTK case study. Cell Chem.Biol. 25 67 PMID: 29129716
If you know of a relevant reference for SJF 1528, please let us know.
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Keywords: SJF 1528, SJF 1528 supplier, SJF1528, protac, degraders, potent, EGFR, epidermal, growth, factor, receptor, ERBB, von, Hippel, Lindau, VHL, E3, ligases, targeted, protein, degradation, TPD, HER2, Active, Degraders, 7262, Tocris Bioscience
Citations for SJF 1528
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Literature in this Area
Tocris offers the following scientific literature in this area to showcase our products. We invite you to request* your copy today!
*Please note that Tocris will only send literature to established scientific business / institute addresses.
Targeted Protein Degradation Research Product Guide
This brochure highlights the tools and services available from Bio-Techne to support Targeted Protein Degradation research, including:
- Active Degraders
- TAG Degradation Platform
- Degrader Building Blocks
- Ubiquitin-Proteasome System Proteins
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Epigenetics Scientific Review
Written by Susanne Müller-Knapp and Peter J. Brown, this review gives an overview of the development of chemical probes for epigenetic targets, as well as the impact of these tool compounds being made available to the scientific community. In addition, their biological effects are also discussed. Epigenetic compounds available from Tocris are listed.
Epigenetics in Cancer PosterUpdated
This poster summarizes the main epigenetic targets in cancer. The dysregulation of epigenetic modifications has been shown to result in oncogenesis and cancer progression. Unlike genetic mutations, epigenetic alterations are considered to be reversible and thus make promising therapeutic targets.
Targeted Protein Degradation Poster
Degraders (e.g. PROTACs) are bifunctional small molecules, that harness the Ubiquitin Proteasome System (UPS) to selectively degrade target proteins within cells. They consist of three covalently linked components: an E3 ubiquitin ligase ligand, a linker and a ligand for the target protein of interest. Authored in-house, this poster outlines the generation of a toolbox of building blocks for the development of Degraders. The characteristics and selection of each of these components are discussed. Presented at EFMC 2018, Ljubljana, Slovenia