MS 154 AC Bcl2 degrader-1 SK-MEL-5 and A375 with IC50

SK-MEL-5 and A375 with IC50 from 2

CAS Number: 1446144-04-2

PubMed PMID: 30271980

Effects of two chemically related new Ca2+ channel antagonists

KDM5-C70 increases H3K4me3 levels in myeloma cells

MS 154 AC Bcl2 degrader-1 SK-MEL-5 and A375 with IC50MS 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