Prexasertib HCl (LY2606368)
Molecular Weight(MW): 438.31
Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.
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|Description||Prexasertib (LY2606368) is an ATP-competitive CHK1 inhibitor with a Ki value of 0.9 nmol/L. For CHK2 and RSK, its IC50 values are 8 nM and 9 nM respectively in cell-free assay.|
In nonclinical studies, LY2606368 induced DNA damage as measured by replication catastrophe and increases in pH2A.X, a marker of double-stranded DNA breaks. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population. In a functional assay, LY2606368 potently abrogated the G2–M checkpoint activated by doxorubicin in p53-deficient HeLa cells with an EC50 of 9 nmol/L. LY2606368 was broadly antiproliferative with IC50 values typically <50 nmol/L in the most sensitive cell lines with a minority of cell lines showing considerable resistance with IC50's >1,000 nmol/L. LY2606368 requires CDC25A and CDK2 to cause DNA damage.
|In vivo||LY2606368 inhibited tumor growth in cancer xenografts as monotherapy and in combination with other agents. In an orthotopic SKOV3 ovarian cancer model, LY2606368 was shown to inhibit the growth of primary tumors and significantly reduce the incidence of metastases and ascites accumulation. LY2606368 also demonstrated efficacy in an SW1990 orthotopic pancreatic cancer model resulting in a 92% inhibition of primary tumor growth and the elimination of metastases to the lymphnode, spleen, and intestine.|
|In vitro||DMSO||2 mg/mL (4.56 mM)|
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02649764||Active not recruiting||Leukemia||M.D. Anderson Cancer Center|Eli Lilly and Company||May 4 2016||Phase 1|
|NCT02203513||Recruiting||Ovarian Cancer|Breast Cancer|Prostate Cancer||National Cancer Institute (NCI)|National Institutes of Health Clinical Center (CC)||July 29 2014||Phase 2|
|NCT02808650||Recruiting||Childhood Solid Neoplasm|Recurrent Central Nervous System Neoplasm|Recurrent Malignant Solid Neoplasm|Refractory Central Nervous System Neoplasm|Refractory Malignant Solid Neoplasm||Children''s Oncology Group|National Cancer Institute (NCI)||February 27 2017||Phase 1|
|NCT02555644||Recruiting||Head and Neck Neoplasms||Eli Lilly and Company||February 24 2016||Phase 1|
|NCT02778126||Active not recruiting||Advanced Cancer||Eli Lilly and Company||September 22 2016||Phase 1|
|NCT02514603||Completed||Neoplasm||Eli Lilly and Company||October 2015||Phase 1|
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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Frequently Asked Questions
What is the solubility of LY2606368 in 20% Captisol?
S7178 in 20% Captisol is a suspension, which is fine for oral gavage. You can dissolve it in this vehicle to the concentration you need as long as the suspension is homogeneous.