Definition

The tosylate salt form of T-1101, an orally bioavailable inhibitor of highly expressed in cancer 1 (Hec1) and NIMA-related kinase 2 (Nek2), with potential antineoplastic activity. Upon oral administration, T-1101 specifically targets, binds to and inhibits the interaction of Hec1 with Nek2. This prevents Hec1/Nek2-mediated signal transduction pathways, inhibits mitosis, induces apoptosis and tumor cell proliferation. Hec1, overexpressed in some cancers, is located at the centromere during cell mitosis and plays an essential role in the pathway of spindle checkpoint. It is correlated with cancer formation, progression, and survival. Phosphorylation of Hec1 by Nek2 kinase is essential for its mitotic function.