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
Powered by Bioz1) Fan, Q., et al. (2006) .”A dual PI3 kinase/mTOR inhibitor reveals emergent efficacy in glioma.” Cancer Cell 9: 341-349.
2) Smit, M. A., T. R. Geiger, et al. (2009). “A Twist-Snail axis critical for TrkB-induced epithelial-mesenchymal transition-like transformation, anoikis resistance, and metastasis.” Mol Cell Biol 29(13): 3722-37.
3) Gursel, D. B., Y. S. Connell-Albert, et al. (2011). “Control of proliferation in astrocytoma cells by the receptor tyrosine kinase/PI3K/AKT signaling axis and the use of PI-103 and TCN as potential anti-astrocytoma therapies.” Neuro-Oncology 13(6): 610-621.
