产品描述:
ON-123300 is a multi-kinase inhibitor.{43515,43516} It inhibits ARK5, Cdk4, and Cdk6 (IC50s = 3.87, 9.82, and 4.95 nM, respectively) as well as FYN, PDGFRβ, Abl, and PI3Kδ (IC50s = 11.09, 26, 53.32, and 144 nM, respectively) among others.{43516} It inhibits proliferation in a panel of 38 cancer cell lines (GI50s = 0.05-5 µM).{43516} ON-123300 also inhibits proliferation of U87 glioma cells (IC50 = 3.4 µM), decreases phosphorylation of Akt and activates ERK, as well as halts the cell cycle in the G2/M phase and induces apoptosis.{43515} When used in combination with the EGFR inhibitor gefitinib (Item No. 13166), it synergistically induces cytotoxicity of U87, U87 VIII, and U87 PTEN cells. ON-123300 reduces tumor growth in an MDA-MB-231 mouse xenograft model when administered at a dose of 50 mg/kg every other day.{43516}