SJF 1521

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Description: Selective EGFR PROTAC® Degrader
Chemical Name: (2S,4R)-1-((S)-2-(tert-Butyl)-14-(4-(4-((3-chloro-4-((3-fluorobenzyl)oxy)phenyl)amino)quinazolin-6-yl)phenoxy)-4-oxo-6,9,12-trioxa-3-azatetradecanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide
Purity: ≥98% (HPLC)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity for SJF 1521

SJF 1521 is a selective EGFR PROTAC® Degrader. SJF 1521 comprises the EGFR inhibitor lapatinib (Cat. No. 6811) joined by a linker to a von Hippel-Lindau (VHL) recruiting ligand. Exhibits selectivity for EGFR, including mutant forms, over HER2. Induces degradation of EGFR in OVCAR8 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.

Technical Data for SJF 1521

M. Wt 1074.66
Formula C57H61ClFN7O9S
Storage Store at -20°C
Purity ≥98% (HPLC)
CAS Number 2230821-40-4
PubChem ID 135157094
InChI Key XZNORRXEBCTXPB-KHBXAZQSSA-N
Smiles CC1=C(C2=CC=C(C=C2)CNC([C@@H]3C[C@H](CN3C([C@H](C(C)(C)C)NC(COCCOCCOCCOC4=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 1521

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 107.47 100

Preparing Stock Solutions for SJF 1521

The following data is based on the product molecular weight 1074.66. 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.

Select a batch to recalculate based on the batch molecular weight:
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 0.93 mL 4.65 mL 9.31 mL
5 mM 0.19 mL 0.93 mL 1.86 mL
10 mM 0.09 mL 0.47 mL 0.93 mL
50 mM 0.02 mL 0.09 mL 0.19 mL

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References for SJF 1521

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 1521, please let us know.

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Citations for SJF 1521

Citations are publications that use Tocris products.

Currently there are no citations for SJF 1521. Do you know of a great paper that uses SJF 1521 from Tocris? Please let us know.

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Literature in this Area

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Targeted Protein Degradation Research Product Guide

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
  • Assays for Protein Degradation
Targeted Protein Degradation Poster

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