PI-103 is a cell-permeable pyridinylfuranopyrimidine compound that acts as an ATP-competitive inhibitor of DNA-PK, PI 3-kinase (Class IA), and FRAP (mTOR) complex 1 and 2. Studies suggest that PI-103 can induce apoptosis and an arrest in the cell cycle by inhibition of the aforementioned proteins. When PI-103 is combined with rapamycin, a prototypic mTORC1 inhibitor, synergistic suppression of AKT and ribosomal S6 protein phosphorylation are observed. In addition, PI-103 has been seen to have nominal effects inhibiting basal Na+ transport, but is very effective in abolishing insulin-induced Na+ absorption in the nephron.
1. Demyanets, S., et al. 2010. Basic Res Cardiol. [Epub ahead of print]. PMID: 21174212 2. Mansley, M.K., et al. 2010. Br. J. Pharmacol. 161: 571-588. PMID: 20880397 3. Bagci-Onder, T., et al. 2010. Cancer Res. [Epub ahead of print]. PMID: 21084267 4. Werzowa, J., et al. 2010. J. Invest. Dermatol. [Epub ahead of print]. PMID: 21048785
Soluble in DMSO (10 mg/ml), DMF (10 mg/ml), 1:2 DMSO:PBS(pH 7.2) (0.25 mg/ml), water (<1 mg/ml) at 25° C, and ethanol (<1 mg/ml) at 25° C.
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FanFan, QW. et al. (PubMed 17804702) used PI-103, an ATP-competitive dual inhibitor of Class IA PI3K and mTOR complex 1 and 2, to increase the efficacy of erlotinib against EGFR-driven glioma cell lines containing mutant PTEN. Introduction of PI-103 significantly increased erlotinib anti-proliferative efficacy in mutant PTEN glioma cell lines. -SCBT Publication Review
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