SNS-314

SNS-314 is a potent and selective aurora kinase inhibitor with IC₅₀s of 9, 31, and 6 nM for aurora A, B and C, respectively^[1]. In Vitro: SNS-314 blocks proliferation in a broad panel of tumor cell lines (HCT116, A2780, PC-3, HeLa, MDA-MB-231, H-1299, and HT29) with IC₅₀ values ranging from 1.8 nM in A2780 ovarian cancer cells to 24 nM in HT29 colon cancer cells^[2]. In Vivo: In the HCT116 human colon cancer xenograft model, administration of 50 and 100 mg/kg SNS-314 leads to dose-dependent inhibition of histone H3 phosphorylation for at least 10 h. SNS-314 shows significant tumor growth inhibition in a dose dependent manner under a variety of dosing schedules including weekly, bi-weekly, and 5 days on/9 days off^[2].