AT-9283

AT-9283 is a broad spectrum kinase inhibitor that potently inhibits Aurora A, Aurora B, JAK2, JAK3, and c-ABL (IC₅₀s = 3, 3, 1.2, 1.1, and 4 nM, respectively).¹ It also potently (IC₅₀ = <1 μM) inhibits many other kinases, including serine/threonine kinases as well as receptor and non-receptor tyrosine kinases.¹ As Aurora kinases have roles in mitosis, inhibitors of these kinases, including AT-9283, have potential in cancer therapy.² Consistent with this, AT-9283 is effective in preventing proliferation of cancer cells both in vitro and in vivo and this effect may be enhanced by combination therapy with other chemotherapeutics.^3,4

WARNING This product is not for human or veterinary use.

1. Howard, S., Berdini, V., Boulstridge, J.A., et al. Fragment-based discovery of the pyrazol-4-yl urea (AT9283), a multitargeted kinase inhibitor with potent aurora kinase activity. J. Med. Chem. 52(2), 379-388 (2009).

2. Curry, J., Angove, H., Fazal, L., et al. Aurora B kinase inhibition in mitosis: Strategies for optimising the use of aurora kinase inhibitors such as AT9283. Cell Cycle 8(12), 1921-1929 (2009).

3. Qi, W., Liu, X., Cooke, L.S., et al. AT9283, a novel aurora kinase inhibitor, suppresses tumor growth in aggressive B-cell lymphomas. Int. J. Cancer 130(12), 2997-3005 (2012).

4. Santo, L., Hideshima, T., Cirstea, D., et al. Antimyeloma activity of a multitargeted kinase inhibitor, AT9283, via potent Aurora kinase and STAT3 inhibition either alone or in combination with lenalidomide. Clin. Cancer Res. 17(10), 3259-3271 (2011).