MS 154 AC Bcl2 degrader-1 Johanna Kastl et al

Johanna Kastl et al

Effects of two chemically related new Ca2+ channel antagonists

PubMed PMID: 30271980

7 macrophages in vitro at a dosage of 10μM

Formula: C18H14Cl2N2O2

MS 154 AC Bcl2 degrader-1 Johanna Kastl et alMS 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