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Biological Activity:
Potent and selective inhibitor of Aurora A kinase (AurA), with IC50 values to be 4.3 nM (Aurora A) and unusually high selectivity 860 fold against Aurora B; a useful tool compound for investigating the cellular role of Aurora A kinases.
This ligand has much higher selectivity of Aurora A vs Aurora B than another recently described relatively selective Aurora A inhibitor MLN8054, which shows 43-fold selectivity for Aurora A over Aurora B in enzymatic assays.
References:
I Aliagas-Martin et al. A class of 2,4-bisanilinopyrimidine Aurora A inhibitors with unusually high selectivity against Aurora B. J. Med. Chem. 2009, 52(10), 3300-7. [online]
Chemical Name: 4-(2-{4-[2-(4-Acetyl-piperazin-1-yl)-2-oxo-ethyl]-phenylamino}-5-fluoro-pyrimidin-4-ylamino)-N-(2-chloro-phenyl)-benzamide
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