Cellular IC50 (nM) of imatinib (IM), nilotinib (NI), and dasatinib (DA) and fold increase with respect to the IC50 for wild-type (WT) Bcr-Abl of the M244V, L248V, G250E, Q252H, Y253H, Y253F, E255K, E255V, E279K, and V299L mutant forms
Data were collated from 10 published studies. a, Shah et al6 ; b, Corbin et al11 ; c, Azam et al73 ; d, O'Hare et al24 ; e, Burgess et al47 ; f, Manley et al74 ; g, Weisberg et al26 ; h, Bradeen et al75 ; i, Ray et al76 ; and l, Redaelli et al.77 Mouse lymphoblastoid cells (BaF3) transfected with p210BCR-ABL were used in all the studies. The IC50 was calculated with different methods, namely, trypan blue exclusion,6,26,47,76 MTT,11 WST-1,73 or MTS24,76 colorimetric assays, ATP-lite fluorescent assay,26,74 and tritiated thymidine incorporation.77 In one study75 the method was not detailed. IC50 was assessed after 48,6,11 60,73 70,26,74 or 7224,47,76 hours of incubation with the inhibitors. In the other studies,75,77 this information was not provided.
