Highly potent, ATP-competitive inhibitor selective for Aurora A kinase (Ki = 0.3 nM; IC50 = 6.7 nM) over Aurora B (IC50 = 1.5 µM); does not inhibit a large panel of other kinases. Also exhibits off-target binding of GABAA (IC50 = 0.49 µM), but no effects attributable to this binding were...
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Highly potent, ATP-competitive inhibitor selective for Aurora A kinase (Ki = 0.3 nM; IC50 = 6.7 nM) over Aurora B (IC50 = 1.5 µM); does not inhibit a large panel of other kinases. Also exhibits off-target binding of GABAA (IC50 = 0.49 µM), but no effects attributable to this binding were observed in rats. Disrupts the Aurora A / Myc complex, resulting in Myc degradation in Myc-amplified neuroblastomas. Inhibits tumor cell growth in vitro and in vivo, causing apoptosis and autophagy, disrupted mitosis, and increased chromosome alignment abnormalities
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