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. 2016 Nov 2;21(11):1462. doi: 10.3390/molecules21111462

Table 1.

In vitro EGFR tyrosine kinases (wild-type and L858R/T790M mutation) activities a.

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).