sjf-1528

Potent EGFR 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. 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).

SJF-1528 hemihydrate 是 SJF-1528 的半水合物形式。这种化合物是 EGFR PROTAC 降解剂，在 OVCAR8 细胞中对野生型 EGFR 和在 HeLa 细胞中对外显子 20 Ins 突变型 EGFR 具有活性，DC50 分别为 39.2 nM 和 736.2 nM。SJF-1528 hemihydrate 还可降解 HER2。