Uses
MS9427 is a potent PROTAC EGFR degrader with Kds 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[1].
IC 50
EGFR (WT): 7.1 nM (Kd); EGFR L858R: 4.3 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