DDC-01-163

DDC-01-163 is an allosteric EGFR degrader that selectively inhibit the proliferation of L858R/T790M (L/T) mutant Ba/F3 cells while leaving wildtype EGFR Ba/F3 cells unaffected;DDC-01-163 exhibited an acceptable biochemical potency with an IC50 value of 45 nM against EGFR L858R/T790M.DDC-01-163 is also effective against osimertinib-resistant cells with L/T/C797S and L/T/L718Q EGFR mutations.The anti-proliferative activity of DDC-01-163 against L858R/T790M EGFR-Ba/F3 cells is enhanced when combined with an ATP-site EGFR inhibitor, Osimertinib.

1. Jaebong Jang, et al. Angew Chem Int Ed Engl. 2020 Aug 17;59(34):14481-14489.