egfr (cell: hcc827)

MS 39 is a highly effective, highly affinity and selective depressant of mutant epidermal growth factor receptor (EGFR) with high efficiency, high affinity and selectivity. MS 39, conjured by gefitinib to VHL ligand via a linker, effectively induced the degradation of mutant EGFR (DC50 values in HCC827(exon 19 del) and H3255 (L858R mutation) lung cancer cell lines were 5 nM and 3.3 nM, respectively). However, there was no significant effect in wild-type EGFR cell lines with concentrations up to 10 μM. MS 39 inhibited the proliferation of H3255 lung cancer cells in vitro and was bioavailable in mice after administration.

PROTAC EGFR degrader 4 is a potent molecule designed to target and degrade mutant EGFR, effectively inducing degradation of EGFR del19 and EGFR L858R/T790M with DC50 values of 0.51 nM and 126 nM, respectively. It significantly inhibits the growth of HCC827 and H1975 cell lines, demonstrating IC50 values of 0.83 nM and 203.1 nM, respectively. The induced degradation of EGFR by this compound is associated with autophagy [1].

PROTAC EGFR Degrader 5 (Compound 10), a potent degrader of EGFR Del19 in HCC827 cells, achieves this with a DC50 of 34.8 nM. This compound effectively induces apoptosis in HCC827 cells and causes cell cycle arrest in the G1 phase [1].

PROTAC EGFR degrader 8 (T-184) is a PROTAC that selectively degrades the epidermal growth factor receptor (EGFR) with a DC50 of 15.56 nM in HCC827 cells, and inhibits the growth of cell lines H1975, PC-9, and HCC827 with IC50 values of 7.72 nM, 121.9 nM, and 14.21 nM, respectively. This compound is used primarily for cancer research, particularly in the context of non-small cell lung cancer (NSCLC) [1].