ZSTK474 is an inhibitor of PI3K γ (IC50 at 6 nM). This agent inhibits PI3K α and PI3K β with IC50 of 17 and 53 nM, respectively. ZSTK474 was identified from a chemical library of about 1500 triazine derivatives, and selected for their ability to block tumor cell growth. In preclinical studies ZSTK474 was orally administered to mice and displayed a strong anti-tumoral activity in xenograft models. Toxicity was reported to be moderate. [1]
参考文献
Targeting phosphoinositide 3-kinase—Moving towards therapy Romina Marone,Vladimir Cmiljanovic,et al. Biochimica et Biophysica Acta 2008;1784: 159–185
Antitumor Activity of ZSTK474, a New Phosphatidylinositol 3-Kinase Inhibitor Shin-ichi Yaguchi , Yasuhisa Fukui , et al. Journal of the National Cancer Institute April 19, 2006;98:545-556
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We treated all of drugs in T47D which has a PI3KCA H1044R mutation with the concentration shown below for 1 hour and performed western blot analysis using antibodies to phospho-AKT(SERINE 472), and total AKT.
Western blot analysis of Akt and p-Akt. 0-20μM ZSTK474 was added.
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