T-1101 tosylate (TAI-95 tosylate) is a potent, orally abioavailable Hec1 inhibitor that disrupts Hec1-Nek2 protein interaction wide anti-cancer spectrum (GI50=14.29-73.65 nM, breast cancer cell lines).
A potent, relatively selective Nek2 inhibitor with IC50 of 82.74 nM in cell-free assays; inhibits only 3 kinases (YSK4, FLT3-ITDD835V and FLT3-ITDF691L) against 97 kinases with >65% inhibition at 15 nM; blocks NEK2-EZH2 complex formation and inhibits tumor cell proliferation; efficiently attenuates GBM growth in mouse model and exhibits a synergistic effect with radiotherapy.