SCH 1473759

SCH 1473759 is a novel sub-nanomolar Aurora A/B inhibitor with IC50 of 4 nM and 13 nM, respectively. SCH 1473759 was active against a large panel of tumor cell lines from different tissue origin and genetic backgrounds. SCH-1473759 showed efficacy and target engagement in A2780 human tumor xenograft model in mouse, and also acceptable pharmacokinetic dosing in dog, monkey and rodents, on target efficacy, as well as a safety profile in dogs. SCH 1473759 demonstrated potent mechanism-based activity, and activity was shown to be enhanced in combination with taxanes and KSP inhibitors.