PI-103 is a selective inhibitor for the α-isoform of PI 3-Kinase (IC₅₀: PI 3-Kα = 8 nM, PI 3-Kβ = 88 nM, PI 3-Kδ = 48 nM, PI 3-Kγ = 150 nM). It is also inhibits DNA-PK (IC₅₀ = 2 nM) and mTOR1 and mTOR2 (IC₅₀ = 20 & 83 nM). PI-103 shows little activity against a wide array of protein kinases at 10μM. PI-103 blocks glioma proliferation by blocking the PI 3-K/Akt pathway in vitro and in vivo.

References

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