NTRC 0066-0 is an orally available, selective and potent inhibitor of threonine tyrosine kinase (TTK) that inhibits phosphorylation of TTK substrates and induces chromosome missegregation in cell lines and mice for cancer research.

TTK:0.9 nM

METHODS: To determine the potential relationship between aneuploidy, CIN, and sensitivity to TTK inhibitors, three cell lines that were relatively sensitive to NTRC 0066-0 and three less sensitive cell lines (colon cancer cell line HCT 116, colorectal adenocarcinoma cell line LoVo, and glioblastoma cell line A-172; cervical cancer cell line DoTc2 4520, osteosarcoma cell line MG-63, and ovarian adenocarcinoma cell line OVCAR-3 were selected in a broad cell panel screen and cell proliferation was measured.
RESULTS: Colon cancer cell line HCT 116, colorectal adenocarcinoma cell line LoVo, and glioblastoma cell line A-172 were relatively sensitive to NTRC 0066-0, with IC50 values ​​of 37 nM, 40 nM, and 51 nM, respectively. Cervical cancer cell line DoTc2 4520, osteosarcoma cell line MG-63, and ovarian adenocarcinoma cell line OVCAR-3 were less sensitive, with IC50 values ​​of 117 nM, 135 nM, and 872 nM, respectively. [2]