Table 1.
Compounds | EGFR (IC50, nM) b | SI(WT:L858R/T790M) | |
---|---|---|---|
WT | L858R/T790M | ||
DY3002 | 448.7 | 0.71 | 632.0 |
Rociletinib | 460.2 | 21.5 | 21.4 |
Osimertinib | 482.3 | 11.8 | 40.9 |
Gefitinib | 15.5 | 823.3 | -- |
a Data represent the mean of at least three separate experiments; b Concentration needed to inhibit the autophosphorylation of the cytoplasmic domain of EGFR by 50%, as calculated using GraphPad Prim version 5.0 (GraphPad Software, Inc., La Jolla, CA, USA).