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 9 Publications
5 Customer Reviews
BxPC-3 cells were treated with vehicle control, MK-1775 (MK), LY2603618 (LY) or MK-1775 plus LY2603618 for 48 h. Protein extracts were subjected to Western blotting and probed with anti-PARP, -p-CHK1, -CHK1, -p-CDC25C, -p-CDK1, -CDK1, -p-CDK2, -CDK2, -γH2AX, or -β-actin antibody.
Cancer Lett 2014 10.1016/j.canlet.2014.10.015. Rabusertib (LY2603618) purchased from Selleck.
MK-1775 and LY2603618 synergize to induce apoptosis in AML cell lines and primary patient samples. U937 and CTS cells were treated for 8 h. Whole cell lysates were subjected to Western blotting and probed with anti-γH2AX, -pCHK1, -p-cdc25c, -p-CDK1, -p-CDK2, -CDK1, or -β-actin antibody. Densitometry measurements, as described in the Materials and methods section, are shown below the corresponding Western blot.
J Hematol Oncol 2014 7, 53. Rabusertib (LY2603618) purchased from Selleck.
Biomarker changes induced in response to gemcitabine plus Chk1 inhibitor treatment in HT29 colon carcinoma cells. HT29 colon cancer cells were exposed to 50 nM gemcitabine (+) for 16 hours followed by increasing concentrations of Chk1 inhibitor for a further 24 hours. Protein expression was characterized by immunoblotting.
BMC Cancer 2014 14, 483. Rabusertib (LY2603618) purchased from Selleck.
C6 cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, LY2603618 was added at final concentrations of 0, 1, 5, 10 and 20uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using pS345-CHK1, g-H2AX and beta-actin (internal control) antibodies.
Customer W, F. Z. Rabusertib (LY2603618) purchased from Selleck.
Hela cell was trypsinized and plated at 30% confluence in DMEM. 16 hours later, LY2603618 was added at final concentrations of 0, 5, 10 and 25uM. Another 24 hours later, cells were harvested in RIPA with protease and phosphatase inhibitor cocktail. Total protein concentration was measured by BCA method. Lysates equivalent to 20ug total protein were subject to Western Blot, using total- CHK1, pS345-CHK1 and beta-actin (internal control) antibodies.
Rabusertib (LY2603618) purchased from Selleck.
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Choose Selective Chk Inhibitors
|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:
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||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01358968||Completed||Cancer||Eli Lilly and Company||June 2011||Phase 1|
|NCT01341457||Completed||Solid Tumors||Eli Lilly and Company||May 2011||Phase 1|
|NCT01296568||Completed||Advanced Cancer||Eli Lilly and Company||February 2011||Phase 1|
|NCT01139775||Completed||Non Small Cell Lung Cancer||Eli Lilly and Company||February 2011||Phase 1|Phase 2|
|NCT00988858||Completed||Non Small Cell Lung Cancer||Eli Lilly and Company||November 2009||Phase 2|
|NCT00839332||Completed||Pancreatic Neoplasms||Eli Lilly and Company||March 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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