TAI-1

TAI-1, an orally active anticancer agent, is a highly potent first-in-class Hec1 inhibitor, with a GI₅₀ of 13.48 nM in K562 cells^[1]. IC50 & Target: GI50: 13.48 nM (in K562 cells)^[1]. In Vitro: TAI-1 disrupts Hec1-Nek2 protein interaction, leads to Nek2 degradation, induces significant chromosomal misalignment in metaphase, and induces apoptotic cell death^[1].
TAI-1 induces cancer cell death through the induction of cleavage of apoptotic proteins Caspase 3 and PARP and degradation of anti-apoptotic proteins MCL-1 and suggests that TAI-1 leads to activation of the apoptotic pathways^[1].
TAI-1 is effective in many cancer cells, such as Chronic myeloid leukemia, Cervical cancer, Breast, metastatic-pleural, invasive ductal carcinoma, Acute myeloid leukemia, Myelogenous leukemia, Colorectal carcinoma cells, with GI₅₀ less than 100 nM^[1].
In Vivo: TAI-1 (20 mg/kg intravenously IV/ or 150 mg/kg per oral PO/BID) inhibits tumor growth in multiple cancer xenograft models^[1].