NTRC 0066-0 是一种选择性苏氨酸酪氨酸激酶 (TTK) 抑制剂 (IC50=0.9 nM)。NTRC 0066-0可用于癌症研究。
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].
NTRC 0066-0 has a low selectivity entropy and a relatively long target residence time on TTK and inhibits the proliferation of diverse cancer cell lines with a potency in the same range as that of classic chemotherapeutic agents such as doxorubicin. NTRC 0066-0, has subnanomolar potency in a TTK enzyme assay and inhibits the proliferation of cancer cell lines from diverse tumor tissue origin with IC50 from 11 to 290 nM at 5-day incubation time[1].
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].
[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.
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