AZD-7762 hydrochloride

Checkpoint kinases CHK1 and CHK2 are activated in response to DNA damage that results in cell cycle arrest, allowing sufficient time for DNA repair. Agents that lead to abrogation of such checkpoints have potential to increase the efficacy of such compounds as chemo- and radiotherapies. AZD7762 is a specific inhibitor for the CHK1/2 kinases with IC(50) values less than 10. AZD7762 enhances radiation sensitivity and gemcitabine-mediated radiosensitization in pancreatic cancer cells and xenografts and thus is helpful in the treatments of potentially many cancers. In addition, AZD7762 is a chemosensitizer and with gemcitabine and radiation produced a significant delay in the growth of pancreatic tumor xenografts with tolerable toxicity. AZD7762 is being studied as an important link in improving both adjuvant therapy and the treatment of metastatic disease.