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Alternative Names: PI-103
PI 103 was first described as part of a drug discovery program to develop PI 3-kinase inhibitors (compound 10e in ) and its activity against PI 3-kinase isoforms and other protein kinases has been extensively investigated [1-4]. It is recommended for use as a broad spectrum PI 3-kinase inhibitor .
1 Hayakawa, M., Kaizawa, H., Moritomo, H., Koizumi, T., Ohishi, T., Yamano, M., Okada, M., Ohta, M., Tsukamoto, S., Raynaud, F. I., Workman, P., Waterfield, M. D. and Parker, P. (2007) Synthesis and biological evaluation of pyrido[3',2':4,5]furo[3,2-d]pyrimidine derivatives as novel PI3 kinase p110alpha inhibitors.Bioorganic Medicinal Chemistry Letters 17, 2438-2442
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
3 Knight, Z. A., Gonzalez, B., Feldman, M. E., Zunder, E. R., Goldenberg, D. D., Williams, O., Loewith, R., Stokoe, D., Balla, A., Toth, B., Balla, T., Weiss, W. A., Williams, R. L. and Shokat, K. M. (2006) A pharmacological map of the PI3-K family defines a role for p110a in insulin signalling.Cell 125, 1-15
4 Bain, J., Plater, L., Elliott, M., Shpiro, N., Hastie, C. J., McLauchlan, H., Klevernic, I., Arthur, J. S., Alessi, D. R. and Cohen, P. (2007) The selectivity of protein kinase inhibitors: a further update.Biochem J 408, 297-315