Cayman ON-123300

ON-123300 is a multi-kinase inhibitor.^1,2 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.² It inhibits proliferation in a panel of 38 cancer cell lines (GI₅₀s = 0.05-5 µM).² 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.¹ 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.²

WARNING This product is not for human or veterinary use.