Pdh326 Case Study

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IC50: 8 nM for c-abl

PD 166326 is a receptor tyrosine kinase inhibitor.

Receptor tyrosine kinases are the high-affinity cell surface receptors for many growth factors, cytokines, as well as hormones. They have been shown not only to be critical regulators of normal cellular processes but also to have a key role in the development of many types of cancer.

In vitro: PD 166326 was identified as a pyridopyrimidine-type inhibitor of receptor tyrosine kinases inhibiting c-abl and Bcr/Abl-dependent cell growth. In addition, PD 166326 could also potently inhibit c-src. Moreover, PD166326 was found to be superior to imatinib mesylate in inhibiting the constitutive tyrosine phosphorylation of numerous leukemia-cell proteins,
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