Description
NTRC-0066-0 is a a highly potent and selective small molecule inhibitor of TTK. In cell lines and in mice, NTRC 0066-0 inhibits the phosphorylation of a TTK substrate and induces chromosome missegregation. NTRC 0066-0 inhibits tumor growth in MDA-MB-231 xenografts as a single agent after oral application. The combination of NTRC 0066-0 with a therapeutic dose of docetaxel resulted in doubling of mouse survival and extended tumor remission, without toxicity.
Uses
NTRC 0066-0 is a selective threonine tyrosine kinase (TTK) inhibitor (IC50=0.9 nM). NTRC 0066-0 can be used for the research of cancer[1].
in vivo
NTRC 0066-0 inhibited tumor growth in a mouse xenograft model of the human triple-negative breast cancer (TNBC) cell line MDA-MB-231[1].
References
[1] Uitdehaag JCM, et al. Target Residence Time-Guided Optimization on TTK Kinase Results in Inhibitors with Potent Anti-Proliferative Activity. J Mol Biol. 2017;429(14):2211-2230. DOI:
10.1016/j.jmb.2017.05.014
