Catalog No.S2626 Synonyms: IC-83
Molecular Weight(MW): 436.3
Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.
Cited by 30 Publications
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|Description||Rabusertib (LY2603618) is a highly selective Chk1 inhibitor with potential anti-tumor activity in a cell-free assay. IC50=7 nM, showing approximately 100-fold more potent against Chk1 than against any of the other protein kinases evaluated.|
Chk1 is an ATP-dependent serine-threonine kinase and a key component in the DNA replication-monitoring checkpoint system activated by double-stranded breaks (DSBs). Chk1 contributes to all currently defined cell cycle checkpoints, including G1/S, intra-S-phase, G2/M, and the mitotic spindle checkpoint. By inhibiting the activity of chk1, LY2603618 prevents the repair of DNA caused by DNA-damaging agents, thus potentiating the antitumor efficacies of various chemotherapeutic agents. However, preclinical data involving LY2603618 has not been published until now.  Inhibition of Chk1 is predicted to enhance the effects of antimetabolites, such as gemcitabine.  LY2603618 treatment impairs DNA synthesis, increases DNA damage (via mitotic defects), induces apoptosis, and has synergistic activity with pemetrexed, especially in p53 mutant tumor cells. 
|In vivo||In xenograft models, LY2603618 delays tumor growth when given in combination with pemetrexed. |
|In vitro||DMSO||13 mg/mL (29.79 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+30% PEG400+0.5% Tween80+5% Propylene glycol
For best results, use promptly after mixing.
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01341457||Completed||Drug: LY2603618|Drug: Gemcitabine||Solid Tumors||Eli Lilly and Company||May 2011||Phase 1|
|NCT01296568||Completed||Drug: LY2603618|Drug: Pemetrexed|Drug: Gemcitabine||Advanced Cancer||Eli Lilly and Company||February 2011||Phase 1|
|NCT01139775||Completed||Drug: Pemetrexed|Drug: Cisplatin|Drug: LY2603618||Non Small Cell Lung Cancer||Eli Lilly and Company||February 2011||Phase 1|Phase 2|
|NCT00988858||Completed||Drug: LY2603618|Drug: Pemetrexed||Non Small Cell Lung Cancer||Eli Lilly and Company||November 2009||Phase 2|
|NCT00839332||Completed||Drug: LY2603618|Drug: Gemcitabine||Pancreatic Neoplasms||Eli Lilly and Company||February 2009||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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