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LY-2606368 is an inhibitor of checkpoint kinase (CHK) 1. CHK1 is involved in the regulation of cellular response to DNA damage. Inhibitors of CHK1 are being investigated as chemopotentiating agents because of CHK1’s role in establishing DNA damage checkpoints in the cell cycle. LY-2606368 has shown potential as a treatment for squamous cell carcinoma, neuroblastoma, and small-cell lung cancer when used in conjunction with other drugs.
| Cas No. | 1234015-52-1 |
|---|---|
| Purity | ≥98% |
| Formula | C18H19N7O2 |
| Formula Wt. | 365.40 |
| Chemical Name | Prexasertib |
| IUPAC Name | 5-({5-[2-(3-Aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl}amino)-2-pyrazinecarbonitrile |
| Synonym | LY 2606368, LY2606368, Prexasertib |
| Store Temp | -20°C |
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| Ship Temp | Ambient |
| MSDS | |
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| Info Sheet |
Hong D., Infante J., et al. Phase I Study of LY2606368, a Checkpoint Kinase 1 Inhibitor, in Patients With Advanced Cancer. J Clin Oncol. 34(15):1764-71 (2016). PMID: 27044938.
King C., Diaz H., et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 14(9):2004-13 (2015). PMID: 26141948.
Sen T., Tong P., et al. CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib. Cancer Res. 77(14):2870-84 (2017). PMID: 28490518.
Lowery C., VanWye A., et al. The Checkpoint Kinase 1 Inhibitor Prexasertib Induces Regression of Preclinical Models of Human Neuroblastoma. Clin Cancer Res. 23(15):4354-63 (2017). PMID: 28270495.