LY2603618
Chk1 inhibitor / LY2603618 is a potent (IC50 = 7nM) and selective (>1000x over Chk2) Checkpoint kinase 1 (Chk1) inhibitor.1 Chk1 is an important regulator of the DNA damage response – combination treatment of LY2603618 with other chemotherapeutic agents significantly increased tumor growth inhibition when compared to chemotherapeutic alone.2,3,4 LY2603618 caused a dramatic suppression of cell growth in MCF-7 and MDA-MB-231 human breast cancer cells via Chk1 inhibition induced upregulation of replication stress caused by oncogenes.5
Biochemicals & reagents
911222-45-2
Rabusertib
1) King et al. (2014), Characterization and preclinical development of LY2603618: a selective and potent Chk1 inhibitor; Invest.New Drugs, 32 213 2) Calvo et al. (2014), Preclinical analyses and phase I evaluation of LY2603618 administered in combination with pemetrexed and cisplatin in patients with advanced cancer; Invest.New Drugs, 32 955 3) Calvo et al. (2016), Phase I Study of CHK1 Inhibitor LY2603618 in Combination with Gemcitabine in Patients with Solid Tumors; Oncology, 91 251 4) Zhao et al. (2016), Inhibition of CHK1 enhances cell death induced by the Bcl-1-selective inhibitor ABT-199 in acute myeloid leukemia cells; Oncotarget, 7 34785 5) Zhang et al. (2016), Targeting radioresistant breast cancer cells by single agent CHK1 inhibitor via enhancing replication stress; Oncotarget, 7 34688
-20°C
TARGET: Kinase -- PATHWAY: Cell cycle; DNA damage; Autophagy -- RESEARCH AREA: Cell death -- DISEASE AREA: Cancer