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Prexasertib
$76 – $520
Products Details
Product Description
– 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 <1 nM. Prexasertib inhibits CHK2 (IC50=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].
Web ID
– HY-18174
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– Cancer-Kinase/protease
Molecular Formula
– C18H19N7O2
Citations
– 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.|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.|Sci Rep. 2021 Feb 4;11(1):3176.|Thorax. 2021 Jul 5;thoraxjnl-2021-217377.|Universität Hamburg. Elektronische Dissertationen und Habilitationen. 2022 Aug.|bioRxiv. September 10, 2021.|Methods Mol Biol. 2018;1711:351-398.
References
– [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.
CAS Number
– 1234015-52-1
Molecular Weight
– 365.39
Compound Purity
– 98.74
SMILES
– NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2
Clinical Information
– Phase 2
Research Area
– Cancer
Solubility
– DMSO : 16.67 mg/mL (ultrasonic)
Target
– Apoptosis;Checkpoint Kinase (Chk)
Isoform
– Chk1;Chk2
Pathway
– Apoptosis;Cell Cycle/DNA Damage
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
