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MS9449 is a potent PROTAC EGFR degrader with Kds of 17 nM and 10 nM for EGFR WT and EGFR L858R, respectively. MS9449 effectively induces degradation of mutant EGFRs through both the ubiquitin/proteasome system (UPS) and autophagy/lysosome pathways. MS9449 potently inhibits the proliferation of NSCLC cells. MS9449 can be used for researching anticancer[1]. | [IC 50]
EGFR (WT): 17 nM (Kd); EGFR L858R: 10 nM (Kd) | [References]
[1] Yu X, et al. Exploring Degradation of Mutant and Wild-Type Epidermal Growth Factor Receptors Induced by Proteolysis-Targeting Chimeras. J Med Chem. 2022 Jun 23;65(12):8416-8443. DOI:10.1021/acs.jmedchem.2c00345 |
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