| References: |
LY2606368 is a potent and selective ATP competitive inhibitor(IC50=1.5 nM in SW1990 cell) of the Chk1 protein kinase.LY2606368 alone significantly inhibited the cell proliferation in a variety of pancreatic cell lines (SW1990, SU86.86, Bx-PC3, AsPC-1, CFPAC-1, Capan-2, HPAF-II) with SW1990 being the most sensitive (IC50=1.5 nM).
LY2606368 has been reported to inhibit Chk1 auto-phosphorylation activated by DNA damaging agents, and induce phosphorylation of H2AX, a DNA damage maker in multiple cancer cell lines in vitro. In addition, LY2606368 has demonstrated potent single agent activity and potentiates the anti-tumor activity of DNA damaging agents in vivo. Pancreatic cancer is one of the least curable cancers, with an approximate 5% overall 5-year survival for all patients. In SW1990 pancreas orthotopic model, which represents the local and metastatic growth pattern seen in pancreas cancer patients, LY2606368 treatment resulted in over 92% inhibition of primary tumor growth as well as 100% inhibition of metastasis to lymph node, spleen and intestine. The anti-tumor effect of LY2606368 treatment was further demonstrated in comparing with gemcitabine (the standard of care for pancreas cancer patient) in SW1990 orthotopic model. For the detailed information of LY2606368 dihydrochloride, the solubility of LY2606368 dihydrochloride in water, the solubility of LY2606368 dihydrochloride in DMSO, the solubility of LY2606368 dihydrochloride in PBS buffer, the animal experiment (test) of LY2606368 dihydrochloride, the cell expriment (test) of LY2606368 dihydrochloride, the in vivo, in vitro and clinical trial test of LY2606368 dihydrochloride, the EC50, IC50,and affinity,of LY2606368 dihydrochloride, Please contact DC Chemicals. |
