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. Author manuscript; available in PMC: 2014 Feb 1.
Published in final edited form as: Cancer Discov. 2012 Dec 10;3(2):168–181. doi: 10.1158/2159-8290.CD-12-0357

Figure 3.

Figure 3

In vitro potency of PKC412 against EGFR T790M. A, Comparison of potency between PKC412 and irreversible EGFR inhibitors on phosphorylation of EGFR T790M. Recombinant EGFR proteins were subjected to autophosphorylation reactions in the presence of the indicated concentrations of PKC412, BIBW2992, HKI-272, or WZ4002. Note that the potency of BIBW2992 and HKI-272 against EGFR wild-type and T790M is similar. B, Assessment of inhibition constant (Ki) values of PKC412 for EGFR T790M. Ki values for recombinant EGFR wild-type, del E746_A750/T790M, or L858R/T790M and fold selectivity over EGFR wild-type were calculated for PKC412. Ki values were calculated as described in Methods.