Prexasertib

• UNSPSC 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 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].

• 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.html

• Purity:

  98.74

• Solubility:

  DMSO : 16.67 mg/mL (ultrasonic)

• Smiles:

  NCCCOC(C=CC=C1OC)=C1C2=CC(NC3=NC=C(C#N)N=C3)=NN2

• Molecular Weight:

  365.39

• 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. 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.|bioRxiv. September 10, 2021.|Methods Mol Biol. 2018;1711:351-398.|Neurooncol Adv. 2024 Nov 19;6(1):vdae187.

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  -20°C, 3 years; 4°C, 2 years (Powder)

• Clinical Information:

  Phase 2

• CAS Number:

  1234015-52-1