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分类

• Approved Therapeutics/Drug Candidates, Cell Biology, Cell Signaling and Neuroscience, Kinase/Phosphatase Biology, Non-Receptor Tyrosine Kinase Biology, Non-Receptor Tyrosine Kinase Inhibitors, Pfizer Compounds, c-Abl
• {SNA} Approved Therapeutics/Drug Candidates, Bioactive Small Molecule Alphabetical Index, Diversification Ready Pharma-Developed Compounds, Kinase/Phosphatase Biology, Non-Receptor Tyrosine Kinase Biology, Non-Receptor Tyrosine Kinase Inhibitors, P-PH, Pfizer Compounds, c-Abl, 生物活性小分子, 细胞信号转导和神经科学, 细胞生物学

产品应用

• PD180970 is a novel Bcr-Abl inhbiitor. PD180970 inhibited in vivo tyrosine phosphorylation of p210Bcr-Abl (IC50 = 170 nM) and the p210BcrAbl substrates Gab2 and CrkL (IC50 = 80 nM) in human K562 chronic myelogenous leukemic cells. In vitro, PD180970 potently inhibited autophosphorylation of p210Bcr-Abl (IC50 = 5 nM) and the kinase activity of purified recombinant Abl tyrosine kinase (IC50 = 2.2 nM). Incubation of K562 cells with PD180970 resulted in cell death. PD180970 is among the most potent inhibitors of the p210Bcr-Abl tyrosine kinase, which is present in almost all cases of human chronic myelogenous leukemia. PD180970 is a promising candidate as a novel therapeutic agent for Bcr-Abl-positive leukemia.

相关文献及参考

• Cowan-Jacob, S.W., et al., Imatinib (STI571) resistance in chronic myelogenous leukemia: molecular basis of the underlying mechanisms and potential strategies for treatment. Mini Rev. Med. Chem. 4 , 285-299, (2004)
• LaRosee, P., et al., Activity of the Bcr-Abl kinase inhibitor PD180970 against clinically relevant Bcr-Abl isoforms that cause resistance to imatinib mesylate (Gleevec, STI571). Cancer Res. 62 , 7149-7155, (2002)

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