Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases

@article{Granda2012BiologicalCO,
  title={Biological characterization of ETP-46321 a selective and efficacious inhibitor of phosphoinositide-3-kinases},
  author={T. Granda and D. Cebri{\'a}n and Sonia Mart{\'i}nez and Patricia Villanueva Anguita and E. Lopez and W. Link and T. Merino and J. Pastor and Beatriz G. Serelde and S. Peregrina and Irene Palacios and M. I. Albarr{\'a}n and A. Cebri{\'a} and Milagros Lorenzo and Patricia Alonso and J. Fominaya and Ana Rodr{\'i}guez Lopez and J. Bischoff},
  journal={Investigational New Drugs},
  year={2012},
  volume={31},
  pages={66-76}
}
SummaryInhibitors of PI3K signaling are of great therapeutic interest in oncology. The phosphoinositide-3-kinase signaling pathway is activated in a variety of solid and non-solid tumors. We have identified an imidazopyrazine derivative, ETP-46321, as a potent inhibitor of PI3Kα $$ {\text{K}}_{\text{i}}^{\text{app}} = {2}.{\text{4 nM}} $$. The compound was 6 times less potent towards PI3Kδ and more than 200 and 60 times less potent at inhibiting PI3Kβ and PI3Kγ and did not significantly inhibit… Expand
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