SJF-1528 hemidrate is the hemidrate form of SJF-1528 . SJF-1528 hemidrate is a EGFR PROTAC degrader with DC50 values of 39.2 nM and 736.2 nM for wild-type EGFR in OVCAR8 cells and Exon 20 Ins mutated EGFR in HeLa cells. SJF-1528 hemidrate also degrades HER2. (Pink: ligand for target protein ; Black: linker Tos-PEG2-CH2-Boc ; Blue: ligand for E3 ligase (S,R,S)-AHPC )
References:
[1]. Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.