Oritinib (SH-1028), an irreversible third-generation EGFR TKI , overcomes T790M-mediated resistance in non-small cell lung cancer . Oritinib (SH-1028), a mutant-selective inhibitor of EGFR kinase activity, inhibits EGFR WT , EGFR L858R , EGFR L861Q , EGFR L858R/T790M , EGFR d746-750 and EGFR d746-750/T790M kinases, with IC 50 s of 18, 0.7, 4, 0.1, 1.4 and 0.89 nM, respectively.
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