Aurora Kinase Inhibitor III

Aurora kinase inhibitor-3 is a strong and selective Aurora A kinase inhibitor with an IC50 of 42 nM, and weakly inhibits EGFR with an IC50 of >10 μM. Aurora kinase inhibitor-3 has a binding mode with the cyclopropanecarboxylic acid moiety directed towards the solvent exposed region of the ATP-binding pocket[1].

A cell-permeable 2,4-dianilinopyrimidine compound that acts as an ATP-competitive, potent, but non-selective inhibitor of Aurora A (IC₅₀ = 42 nM). At higher concentrations, also inhibits the activities of other kinases, such as Lck, Bmx, IGF-1R, and Syk (IC₅₀ = 131, 386, 591, and 887 nM, respectively).

Target IC50: 42 nM against Aurora A; 131, 386, 591, and 887 nM, against Lck, Bmx, IGF-1R, and Syk , respectively

Aurora A: 42 nM (IC₅₀)

[1] Tari LW, et al. Structural basis for the inhibition of Aurora A kinase by a novel class of high affinitydisubstituted pyrimidine inhibitors. Bioorg Med Chem Lett. 2007 Feb 1;17(3):688-91. DOI:10.1016/j.bmcl.2006.10.086