Prexasertib (dihydrochloride)
Product Specifications
UNSPSC Description
Prexasertib dihydrochloride (LY2606368 dihydrochloride) 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 dihydrochloride causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib dihydrochloride shows potent anti-tumor activity[1][2].
Target Antigen
Apoptosis; Checkpoint Kinase (Chk)
Type
Reference compound
Related Pathways
Apoptosis;Cell Cycle/DNA Damage
Applications
Cancer-Kinase/protease
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/LY2606368-dihydrochloride.html
Purity
99.41
Solubility
DMSO : 8 mg/mL (ultrasonic)|H2O : < 0.1 mg/mL
Smiles
NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2.[H]Cl.[H]Cl
Molecular Weight
438.31
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.bioRxiv. September 10, 2021.|Methods Mol Biol. 2018;1711:351-398.|Neurooncol Adv. 2024 Nov 19;6(1):vdae187.|bioRxiv. 2024 Nov 6:2024.11.04.621884.|bioRxiv. January 04, 2022.|Br J Cancer. 2021 Mar 26.|Cancers (Basel). 2021 Aug 20;13(16):4200.|Cancers. 2020 Aug 26;12(9):2426.|Cancers. 2020 Jun 29;12(7):1726.|Cell Biol Toxicol. 2021 Sep 14.|Cells. 2024 Apr 19;13(8):710.|Mol Cancer Res. 2019 Oct;17(10):2102-2114.|Nat Commun. 2019 Aug 2;10(1):3485.|Oncogene. 2022 Oct 12.|Patent. US20210353605A1.|Research Square Preprint. 2021 May.|Research Square Preprint. 2024 Nov 06.|Sci Rep. 2021 Feb 4;11(1):3176.|Thorax. 2021 Jul 5;thoraxjnl-2021-217377.|Universität Hamburg. Elektronische Dissertationen und Habilitationen. 2022 Aug.|Utrecht University. 2023 Feb.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, sealed storage, away from moisture)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-18174A/Prexasertib-dihydrochloride-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-18174A/Prexasertib-dihydrochloride-SDS-MedChemExpress.pdf
Clinical Information
Phase 2
CAS Number
1234015-54-3
Available Sizes
Curated Selection
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