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Prexasertib (mesylate)

CAT: 0804-HY-18174CSize: 1 EachDry Ice: NoHazardous: No
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CAT#:0804-HY-18174CSize:1 Each
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Description
Prexasertib mesylate (LY2606368 mesylate) 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 mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity[1][2].
CAS Number
1234015-55-4
Product Name Alternative
LY2606368 (mesylate)
UNSPSC
12352005
Target
Apoptosis; Checkpoint Kinase (Chk) ; DNA/RNA Synthesis
Type
Reference compound
Related Pathways
Apoptosis; Cell Cycle/DNA Damage
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/prexasertib-mesylate.html
Solubility
10 mM in DMSO
Smiles
N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O
Molecular Formula
C19H23N7O5S
Molecular Weight
461.49
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.
Shipping Conditions
Room temperature
Scientific Category
Reference compound1
Clinical Information
Phase 2
Isoform
Chk1; Chk2

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