PI-103

A cell-permeable pyridinylfuranopyrimidine compound that acts as a potent and ATP competitive inhibitor of DNA-PK, PI3-K, and mTOR (IC50, DNA-PK = 2 nM, p110α = 8 nM , p110β = 88 nM, p110&delta, = 48 nM, p110γ = 150 nM, PI3-KC2b = 26 nM, mTORC1 = 20 nM, and mTORC2 = 83 nM). It inhibits ATR and ATM only at much higher concentrations (IC50 = 850 and 920 nM, respectively) and exhibits little activity towards a panel of more than 40 other kinases even at concentrations as high as 10 µ M. Shown to effectively block PI3-K/Akt signaling and cell proliferation in glioma cell lines both in vitro and in vivo.

371935-74-9

C₁₉H₁₆N₄O₃

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