Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

doi:10.1158/1535-7163.MCT-13-0865

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Characterization of the novel and specific PI3Kα inhibitor NVP-BYL719 and development of the patient stratification strategy for clinical trials.

Molecular cancer therapeutics - 1 May 2014

Fritsch Christine, Huang Alan, Chatenay-Rivauday Christian, Schnell Christian, Reddy Anupama, Liu Manway, Kauffmann Audrey, Guthy Daniel, Erdmann Dirk, De Pover Alain, Furet Pascal, Gao Hui, Ferretti Stephane, Wang Youzhen, Trappe Joerg, Brachmann Saskia M, Maira Sauveur-Michel, Wilson Christopher, Boehm Markus, Garcia-Echeverria Carlos, Chene Patrick, Wiesmann Marion, Cozens Robert, Lehar Joseph, Schlegel Robert, Caravatti Giorgio, Hofmann Francesco, Sellers William R

Abstract excerpt

Somatic PIK3CA mutations are frequently found in solid tumors, raising the hypothesis that selective inhibition of PI3Kα may have robust efficacy in PIK3CA-mutant cancers while sparing patients the side-effects associated with broader inhibition of the class I phosphoinositide 3-kinase (PI3K) family. Here, we report the biologic properties of the 2-aminothiazole derivative NVP-BYL719, a selective inhibitor of...

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PMID: 24608574
DOI: 10.1158/1535-7163.MCT-13-0865

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PTEN

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