4.4 Article

Testing of the Akt/PKB inhibitor MK-2206 by the pediatric preclinical testing program

期刊

PEDIATRIC BLOOD & CANCER
卷 59, 期 3, 页码 518-524

出版社

WILEY
DOI: 10.1002/pbc.23412

关键词

developmental therapeutics; MK-2206; preclinical testing

资金

  1. National Cancer Institute [NO1-CM-42216, CA21765, CA108786]

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Background MK-2206 is a small molecule allosteric inhibitor of Akt/PKB that is undergoing clinical trials for treatment of cancer. Procedures MK-2206 was tested against the PPTP in vitro panel using a 96-hour exposure (1.0?nM10?mu M), and in vivo using thrice weekly dosing for a planned 4 weeks at its maximum tolerated dose (MTD) of 180?mg/kg. Results In vitro, the median relative IC50 value for MK-2206 was 2.2?mu M. Four cell lines with IC50 values?

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