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Comparison of imatinib, dasatinib, nilotinib and INNO-406 in imatinib-resistant cell lines.

Author(s): Deguchi Y, Kimura S, Ashihara E, Niwa T, Hodohara K, Fujiyama Y, Maekawa T

Affiliation(s): Department of Transfusion Medicine and Cell Therapy, Kyoto University Hospital, 54 Kawahara-cho Shogoin Sakyo-ku, Kyoto 606-8507, Japan.

Publication date & source: 2008-06, Leuk Res., 32(6):980-3. Epub 2008 Jan 8.

Publication type: Comparative Study; Research Support, Non-U.S. Gov't

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.

Page last updated: 2008-08-10

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