SJF 1528
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%
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
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
-
The advantages of targeted protein degradation over inhibition: an RTK case study.
Burslem et al.
Cell Chem.Biol., 2018;25:67
Product Datasheets
Reconstitution Calculator
Molarity Calculator
FAQs
No product specific FAQs exist for this product, however you may
View all Small Molecule FAQsReviews for SJF 1528
There are currently no reviews for this product. Be the first to review SJF 1528 and earn rewards!
Have you used SJF 1528?
Submit a review and receive an Amazon gift card.
$25/€18/£15/$25CAN/¥75 Yuan/¥2500 Yen for a review with an image
$10/€7/£6/$10 CAD/¥70 Yuan/¥1110 Yen for a review without an image