Rociletinib (CO-1686, AVL-301, CNX-419) is a potent, highly selective, irreversible inhibitor of mutant EGFR with Ki of 21.5 nM for EGFR L858R/T790M.
Rociletinib shows 22-fold selective over WT EGFR; EGFR del19, T790M, L858R/T790M and L858R mutant kinases demonstrates the highest degree of inhibition at 0.1 uM; orally bioavailable.
Rociletinib (CO-1686) also is a highly potent and specific covalent inhibitor of NEK7, binds to the cysteine 79 of NEK7
