In vivo antiproliferative effect of NS-187, a dual Bcr-Abl/Lyn tyrosine kinase inhibitor, on leukemic cells harbouring Abl kinase domain mutations
H Naito, S Kimura, Y Nakaya, H Naruoka, S Kimura… - Leukemia research, 2006 - Elsevier
Advanced-phase chronic myeloid leukemia patients treated with imatinib often relapse due
to point mutations in the Abl kinase domain. We herein examine the in vitro and in vivo
effects of a Bcr-Abl/Lyn dual tyrosine kinase inhibitor, NS-187, on seven mutated Bcr-Abl
proteins. NS-187 inhibited both Tyr393-phosphorylated and Tyr393-unphosphorylated Abl,
resulting in significant in vitro growth inhibition of cells expressing six of seven mutated Bcr-
Abl kinases, though not T315I. Furthermore, NS-187 prolonged the survival of mice injected …
to point mutations in the Abl kinase domain. We herein examine the in vitro and in vivo
effects of a Bcr-Abl/Lyn dual tyrosine kinase inhibitor, NS-187, on seven mutated Bcr-Abl
proteins. NS-187 inhibited both Tyr393-phosphorylated and Tyr393-unphosphorylated Abl,
resulting in significant in vitro growth inhibition of cells expressing six of seven mutated Bcr-
Abl kinases, though not T315I. Furthermore, NS-187 prolonged the survival of mice injected …
