Biological Activity
OTS514 hydrochloride is a potent TOPK inhibitor with IC50 of 2.6 nM,it induces cell cycle arrest and apoptosis.
in vitro
OTS514 has growth inhibitory effect on five TOPK-expressing renal cancer cell lines VMRC-RCW, Caki-1, Caki-2, 769-P and 786-O with IC50 ranging from 19.9-44.1 nM. OTS514 can effectively inhibit the growth of TOPK-expressing cancer cells with IC50 ranging from 3-46 nM for the growth inhibition of ovarian cancer cells.
in vivo
Mouse xenograft studies (bearing human lung cancer cells) showed that OTS514 has antitumor activity in vivo, but also caused severe hematopoietic cytotoxicity (reduction of red and white blood cells, thrombocytosis). Oral administration of OTS514 significantly prolonged the lifespan of ES-2 abdominally infected xenograft mice.
target
| Target | Value |
TOPK
(Cell-free assay) | 2.6 nM |
