Gefitinib-based PROTAC 3

PROTAC由与VHL配体1连接的吉非替尼组成；在基于细胞的测定中，诱导含有激活突变L858R或外显子19缺失的EGFR降解（DC50s分别为22.3和11.7nM），但不会在≤10μM时诱导野生型EGFR降解。A PROTAC comprised of gefitinib linked to VHL ligand 1; induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion (DC50s = 22.3 and 11.7 nM, respectively) but does not induce degradation of wild-type EGFR at ≤10 μM in cell-based assays.