NMS-P715 is a potent, selective, orally bioavailable Mps1 inhibitor with IC50 of 8 nM, Ki of 0.99 nM.
NMS-P715 displays excellent selectivity in vitro against a panel of 60 kinases at 5 uM.
NMS-P715 selectively reduces cancer cell proliferation, leaving normal cells almost unaffected, promotes massive spindle assembly checkpoint (SAC) in U2OS cells with EC50 of 68 nM.
NMS-P715 causes a reduction in G1 phase and a flattening in G2/M phase of the cell cycle accompanied by histone H3 dephosphorylation, PARP cleavage, and histone H2AX phosphorylation.
NMS-P715 inhibits tumor growth in preclinical cancer models.
