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Background Information:
LY2606368 (Prexasertib) is a clinical -stage, potent and selective ATP competitive inhibitor of the CHK protein kinase. It preferentially acts on CHK1 (with a biochemical Ki of 0.9 nM) over CHK2 and RSK (with Ki of 8 nM and 9 nM, respectively). CHK1 is a protein kinase that regulates the tumor cell’s response to DNA damage often caused by treatment with chemotherapy. In response to DNA damage, CHK1 blocks cell cycle progression in order to allow to repair damaged DNA, thereby limiting the efficacy of chemotherapeutic agents. Inhibiting CHK1 in combination with chemotherapy can enhance tumor cell death by preventing these cells from recovering from DNA damage.
Reference:
1. King C, et al. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-1.
2. Yin Y, et al. Chk1 inhibition potentiates the therapeutic efficacy of PARP inhibitor BMN673 in gastric cancer. Am J Cancer Res. 2017 Mar 1;7(3):473-483.
APIM050187: LY-2606368 (PREXASERTIB) DIHYDROCHLORIDE
CAS No.: 1234015-54-3 (2 x HCl salt).
Molecular Formula: C18H19N7O2?2HCl.
Molecular Weight: 438.3 (Validated by Quantitative Elemental Analysis).
Purity: >99% (HPLC at 214 and 254 nm).
QC: HPLC, 1H-NMR, and Quantitative Elemental Analysis Report.
Solubility: Refer to Certification of Analysis.
Storage: Refer to Certification of Analysis.
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