LY-2606368 (PREXASERTIB) DIHYDROCHLORIDE

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.