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AMN107 is a small molecule tyrosine kinase inhibitor developed, in the
first instance, as a potent inhibitor of BCR-ABL. We tested its effectiveness
against fusion tyrosine kinases TEL-PDGFRbeta and FIP1L1-PDGFRalpha, which cause
chronic myelomonocytic leukemia and hypereosinophilic syndrome, respectively. In
vitro, AMN107 inhibited proliferation of Ba/F3 cells transformed by both
TEL-PDGFRbeta and FIP1L1-PDGFRalpha with IC50 values < 25 nM, and inhibited
phosphorylation of the fusion kinases and their downstream signaling targets.
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