Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background.

@article{Davies2012PreclinicalPO,
  title={Preclinical pharmacology of AZD5363, an inhibitor of AKT: pharmacodynamics, antitumor activity, and correlation of monotherapy activity with genetic background.},
  author={Barry R. Davies and Hannah L. Greenwood and Phillippa Dudley and Claire Crafter and De-Hua Yu and Jingchuan Zhang and Jing Li and Beirong Gao and Qunsheng Ji and Juliana Maynard and S M Ricketts and Darren A. E. Cross and Sabina C. Cosulich and Christine C. Chresta and Ken Page and J. Yates and Clare D Lane and Rebecca H. Watson and Richard K J Luke and Donald Ogilvie and Martin Pass},
  journal={Molecular cancer therapeutics},
  year={2012},
  volume={11 4},
  pages={873-87}
}
AKT is a key node in the most frequently deregulated signaling network in human cancer. AZD5363, a novel pyrrolopyrimidine-derived compound, inhibited all AKT isoforms with a potency of 10 nmol/L or less and inhibited phosphorylation of AKT substrates in cells with a potency of approximately 0.3 to 0.8 μmol/L. AZD5363 monotherapy inhibited the proliferation of 41 of 182 solid and hematologic tumor cell lines with a potency of 3 μmol/L or less. Cell lines derived from breast cancers showed the… CONTINUE READING
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