产品描述:
OTS514 is an inhibitor of lymphokine-activated killer T cell-originated protein kinase (TOPK; IC50 = 2.6 nM), a serine-threonine kinase often overexpressed and transactivated in several types of cancer.{32494,37578} OTS514 (10 nM) selectively inhibits growth of patient-derived acute myeloid leukemia (AML) cells over normal CD34+ cells. It shows similar growth inhibitory effects in multiple small cell lung, kidney, and ovarian cancer cell lines (IC50s = 0.4-42.6 nM).{37579,37580,32493} In vivo, OTS514 (25 and 50 mg/kg) increases survival in a peritoneal mouse dissemination model of ovarian cancer. It also dose-dependently inhibits tumor growth in an A549 mouse xenograft model when administered at doses of 1, 2.5, and 5 mg/kg.{32494}