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SJF 1528

Catalog #: 7262 Datasheet / COA / SDS
Catalog # Availability Size / Price Qty
7262/5
SJF 1528 | CAS No. 2230821-38-0 | Active Degraders
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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%

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Biological Activity

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

M.Wt:
1030.61
Formula:
C55H57ClFN7O8S
Solubility:
Soluble to 100 mM in DMSO
Purity:
≥98%
Storage:
Store at -20°C
CAS No:
2230821-38-0

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.

Background References

  1. The advantages of targeted protein degradation over inhibition: an RTK case study.
    Burslem et al.
    Cell Chem.Biol., 2018;25:67

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