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Prexasertib (lactate)

Prexasertib lactate (LY2606368 lactate) is the lactate form of Prexasertib. Prexasertib lactate is a selective, ATP-competitive second-generation checkpoint kinase 1 (CHK1) inhibitor with a Ki of 0.9 nM and an IC50 of CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib lactate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib lactate shows potent anti-tumor activity[1][2].

Product Specifications

CAS Number

2781996-46-9

Product Name Alternative

LY2606368 (lactate)

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-lactate.html

Smiles

OC([C@@H](O)C)=O.NCCCOC1=C(C2=CC(NC3=NC=C(C#N)N=C3)=NN2)C(OC)=CC=C1

Molecular Formula

C21H25N7O5

Molecular Weight

455.47

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

Frequently Asked Questions

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