Bafetinib is a Lyn and Bcr-Abl Tyrosine Kinase Inhibitor
The treatment of Philadelphia chromosome-positive (Ph+) leukemias has improved markedly. There are some inhibitors of Bcr-Abl tyrosine kinase (TK) that are effective for Ph<sup>+</sup> leukemias. However, resistance to imatinib can develop by various molecular mechanisms. They include Bcr-Abl overexpression, mutations within the imatinib-binding site of Bcr-Abl, expression of a...
Saracatinib (AZD0530) is a potent Src Family Inhibitor
Src is a prototypical non-receptor tyrosine kinase. It also includes c-Yes and Fyn. Src transduces signals that control processes involved in cell proliferation, adhesion, and motility. Clinical evidence supports a link between deregulation of Src activity and tumor progression and metastasis. Src over-expression and activation are associated with numerous...
A 419259 is a Potent Src Inhibitor
Chronic myelogenous leukemia (CML) is a human malignancy and affects hematopoietic progenitor cells. The CML is driven by Bcr-Abl. Additionally, Bcr-Abl is a 210 kDa chimeric tyrosine kinase that transforms fibroblasts, growth factor-dependent hematopoietic cell lines. Bcr-Abl is a constitutively active protein-tyrosine kinase and can stimulate the proliferation and...