Prexasertib-d4

Prexasertib-d4 (LY2606368-d4) is the deuterium labeled Prexasertib (HY-18174) . Prexasertib (LY2606368) is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of 50=8 nM) and RSK1 (IC50=9 nM) . Prexasertib causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib shows potent anti-tumor activity[1][2].

Product Specifications

Product Name Alternative

LY2606368-d4

UNSPSC

12352005

Target

Apoptosis; Checkpoint Kinase (Chk) ; Isotope-Labeled Compounds

Related Pathways

Apoptosis; Cell Cycle/DNA Damage; Others

Field of Research

Cancer

Smiles

NC([2H])([2H])CC([2H])([2H])OC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2

Molecular Formula

C18H15D4N7O2

Molecular Weight

369.41

References & Citations

[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.