In vitro
ON 01910 is a novel polo-like kinase 1 (Plk1) inhibitor and it inhibit PLK1 with IC50 of 9 nM. ON 01910 also shows cytotoxic activity against a variety of human tumor cell lines in vitro. ON 01910 can induce three major abnormalities in tumor cells, including abnormal cell division (irregular chromosomal segregation and cytokinesis), G2-M arrest and apoptosis, and decreased expression of Cdc25C in many tumor cell lines.
In vivo
In rats, single doses of 300 and 600 mg/m 2 of ON01910 produced no toxicity, and 1200 mg/m2 had only slight toxicity. There was no evidence of significant myelotoxicity, neuropathy, or cardiotoxicity in these toxicology studies. In xenograft mouse model systems, ON01910 inhibited the growth of a wide variety of human tumors, including liver, breast, and pancreatic cancers.
Download Datasheet