OTS514 hydrochloride

OTS514 hydrochloride is a potent TOPK inhibitor with IC50 of 2.6 nM,it induces cell cycle arrest and apoptosis.

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.