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PubMed PMID: 30271980
Johanna Kastl et al
BMDMs or THP-1 cells) potently blocks MDP-induced transcription of the inflammatory mediators TNF and interleukin-6 (IL-6) in bone marrow-derived macrophages (BMDMs)
SK-MEL-5 and A375 with IC50 from 2
CAS Number: 1446144-04-2
MS 154 AC Bcl2 degrader-1 PubMed PMID: 30271980MS 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
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