MS 154 AC Bcl2 degrader-1 METM1250T with IC50s of 3

METM1250T with IC50s of 3

and A375 cells

Formula: C18H14Cl2N2O2

Smiles: CCC1=CC2C(=O)C(=COC=2C(CN2CCCCC2)=C1O)C1=NC2=CC=CC=C2S1

MS 154 AC Bcl2 degrader-1 METM1250T with IC50s of 3MS 154 is a potent and selective cereblon recruiting Degrader (PROTAC) of mutant epidermal growth factor receptor (EGFR), comprising a cereblon binding moiety joined by a linker to gefitinib. MS 154 decreases EGFR protein levels, inhibits downstream signaling in and inhibits proliferation of mutant EGFR bearing lung cancer cells (DC50 values are 11 and 25 nM in HCC 827 and H3255 cells, respectively; Dmax > 95% at 50 nM), but not in WT EGFR bearing