MS9427

MS9427 is a potent PROTAC EGFR degrader with K d s of 7.1 nM and 4.3 nM for EGFR WT and EGFR L858R, respectively. MS9427 selectively degrades the mutant but not the WT EGFR through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9427 potently inhibits the proliferation of NSCLC cells. MS9427 can be used for researching anticancer In Vitro MS9427 has antiproliferative activity against HCC-827 cells, with a GI 50 of 0.87 ± 0.27 μM. MS9427 (0-10 μM, 16 h) potently induces EGFR Del19 degradation (DC 50 =82 ± 73 nM) and inhibits EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Western Blot AnalysisCell Line: HCC-827 cells Concentration: 1, 10, 50, 100, 200, 500, 100, and 10000 nM Incubation Time: 16 h Result: Inhibited EGFR phosphorylation (p-EGFR) in a concentration-dependent manner in HCC-827 cells. Western Blot AnalysisCell Line: HCC-827 cells Concentration: 100 nM Incubation Time: 1, 2, 4, 6, 12, 24, 48 h Result: Induced EGFR degradation in a time-dependent manner and through the UPS and autophagy/lysosome system. Form:Solid IC50& Target:EGFR (WT) 7.1 nM (Kd) EGFR L858R 4.3 nM (Kd)

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