2250404-95-4

T-1101 tosylate (TAI-95 tosylate) is the tosylate salt form of T-1101 (HY-120356). T-1101 tosylate is an orally active inhibitor for mitose regulating highly expressed oncoprotein 1 (Hec1). T-1101 tosylate blocks the interaction between Hec1 and NEK2, exhibits cytotoxicity in human liver cancer cells with GI50 of 15-70 nM. T-1101 tosylate induces apoptosis in Huh-7. T-1101 tosylate exhibits antitumor efficacy in mouse models[1].

NEK2

[1] Huang LY, et al., Inhibition of Hec1 as a novel approach for treatment of primary liver cancer. Cancer Chemother Pharmacol. 2014 Sep;74(3):511-20. DOI:10.1007/s00280-014-2540-7
[2] Chuang SH, et al. Discovery of T-1101 tosylate as a first-in-class clinical candidate for Hec1/Nek2 inhibition in cancer therapy. Eur J Med Chem. 2020 Apr 1;191:112118. DOI:10.1016/j.ejmech.2020.112118