[AMN107] The small molecule tyrosine kinase inhibitor AMN107 inhibits TEL-PDGFR{beta} and FIP1L1-PDGFR{alpha} in vitro and in vivo

[Rob]

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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