PIK-75

Background

PIK-75 was developed as part of a PI 3-kinase drug discovery program (Compound 8c in [1]).  PIK75  attenuates insulin stimulation of Akt/PKB in a range of cell types at 100 nM [2]. The compound has been reported to block growth of a range of cell lines with an IC₅₀ value in the region of 50 nM. In vivo studies have shown that  PIK-75, administered at 50 mg/kg, inhibited the growth of HeLa cell xenografts in mice models [1]

References

1        Hayakawa, M., Kawaguchi, K., Kaizawa, H., Koizumi, T., Ohishi, T., Yamano, M., Okada, M., Ohta, M., Tsukamoto, S., Raynaud, F. I., Parker, P., Workman, P. and Water?eld, M. D. (2007) Synthesis and biological evaluation of sulfonylhydrazone- substituted imidazo[1,2-a]pyridines as novel PI3 kinase p110a inhibitors.Bioorganic Medicinal Chemistry 15, 5837-5844

2        Chaussade, C., Rewcastle, G. W., Kendall, J. D., Denny, W. A., Cho, K., Gronning, L. M., Chong, M. L., Anagnostou, S. H., Jackson, S. P., Daniele, N. and Shepherd, P. R. (2007) Evidence for functional redundancy of class IA PI3K isoforms in insulin signalling.Biochem J 404, 449-58