TAK-960 (hydrochloride)

TAK-960 hydrochloride is a novel, investigational, orally bioavailable, potent, and selective PLK1 inhibitor(IC50=1.5 nM) that has shown activity in several tumor cell lines, including those that express multidrug-resistant protein 1 (MDR1).

IC50 value: 1.5 nM

Target: PLK1

in vitro: Consistent with PLK1 inhibition, TAK-960 treatment caused accumulation of G2–M cells, aberrant polo mitosis morphology, and increased phosphorylation of histone H3 (pHH3) in vitro and in vivo.