title: Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines.
abstract: We compared the growth-inhibitory effects and inhibition profile of the SRC family kinases (SFKs) of imatinib, dasatinib, nilotinib and INNO-406. Dasatinib exhibited the strongest potency against BCR-ABL with little selectivity over SFKs. Nilotinib exhibited a weaker affinity than the other inhibitors, but was highly specific for ABL and may be useful for the treatment of P-glycoprotein overexpressing leukemic cells. INNO-406 had an intermediate affinity for BCR-ABL between that of dasatinib and nilotinib, and inhibited only SFKs LCK and LYN among SFKs. Both nilotinib and INNO-406 were potent inhibitors of the dasatinib-resistant T315A, F317L and F317V BCR-ABL mutations.
authors.affiliation: Department of Transfusion Medicine and Cell Therapy, Kyoto University Hospital, 54 Kawahara-cho Shogoin Sakyo-ku, Kyoto 606-8507, Japan.
authors.forename: Yasuyuki
authors.initials: Y
authors.lastname: Deguchi
authors.forename: Shinya
authors.initials: S
authors.lastname: Kimura
authors.forename: Eishi
authors.initials: E
authors.lastname: Ashihara
authors.forename: Tomoko
authors.initials: T
authors.lastname: Niwa
authors.forename: Keiko
authors.initials: K
authors.lastname: Hodohara
authors.forename: Yoshihide
authors.initials: Y
authors.lastname: Fujiyama
authors.forename: Taira
authors.initials: T
authors.lastname: Maekawa
mesh_terms: D001549:Benzamides; D049109:Cell Proliferation / Q000187:drug effects; D000069439:Dasatinib; D019008:Drug Resistance, Neoplasm; D006801:Humans; D000068877:Imatinib Mesylate; D015464:Leukemia, Myelogenous, Chronic, BCR-ABL Positive / Q000188:drug therapy* / Q000473:pathology; D010879:Piperazines / Q000627:therapeutic use*; D047428:Protein Kinase Inhibitors / Q000627:therapeutic use*; D011743:Pyrimidines / Q000627:therapeutic use*; D013844:Thiazoles / Q000627:therapeutic use*; D014407:Tumor Cells, Cultured
chemical_list: D001549:Benzamides; D010879:Piperazines; D047428:Protein Kinase Inhibitors; D011743:Pyrimidines; D013844:Thiazoles; D000068877:Imatinib Mesylate; C498826:nilotinib; C506918:bafetinib; D000069439:Dasatinib