Journal
LEUKEMIA RESEARCH
Volume 30, Issue 11, Pages 1443-1446Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.leukres.2006.01.006
Keywords
NS-187; Bcr-Abl; Lyn; chronic myeloid leukemia; imatimb
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Advanced-phase chronic myeloid leukemia patients treated with imatinib often relapse due to point mutations in the Ab1 kinase domain. We herein examine the in vitro and in vivo effects of a Ber-Abl/Lyn dual tyrosine kinase inhibitor, NS-187, on seven mutated Bcr-Ab1 proteins. NS-187 inhibited both Tyr393-phosphorylated and Tyr393-unphosphorylated Ab1, resulting in significant in vitro growth inhibition of cells expressing six of seven mutated Bcr-Ab1 kinases, though not T315I. Furthermore, NS-187 prolonged the survival of mice injected with leukemic cells expressing all mutated Bcr-Ab1 tested except T315I, and its efficacy correlated well with its in vitro effects. (c) 2006 Elsevier Ltd. All rights reserved.
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