LY2606368 HCl is a selective ATP competitive inhibitor of checkpoint kinase 1 (IC50: 1.5nM in SW1990 cells).

LY2606368 HCl is an ATP-competitive inhibitor of CHK1 and is undergoing clinical trials currently. It inhibits the auto-phosphorylation of CHK1 and induces the phosphorylation of H2AX in cancer cells. In the pancreatic cell line SW1990, LY2606368 HCl significantly inhibits cell proliferation (IC50: 1.5nM). LY2606368 HCl also exerts potent anti-tumor activity in the SW1990 xenograft model. Besides that, in the orthotopic SKVO3 model, the treatment of LY2606368 HCl is found to inhibit tumor growth and reduce the incidence of metastases and accumulation. However, LY2606368 HCl is only administered intravenously due to its poor oral bioavailability [1][2][3].