Prexasertib

• 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].

• Product Name Alternative :

  LY2606368

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  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 :

  98.75

• Solubility :

  DMSO : 16.67 mg/mL (ultrasonic)

• Smiles :

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

• Molecular Formula :

  C18H19N7O2

• Molecular Weight :

  365.39

• Precautions :

  H302, H315, H319, H335

• 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

• Storage Conditions :

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

• Scientific Category :

  Reference compound1

• Clinical Information :

  Phase 2

• Isoform :

  Chk1; Chk2

• Citation 01 :

  BioRxiv. 2024 Nov 6:2024.11.04.621884.|bioRxiv. 2025 April 17.|bioRxiv. January 04, 2022.|Br J Cancer. 2021 Jul;125 (1) :101-111.|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. 2023 Jun;39 (3) :795-811.|Cell Rep. 2025 Apr 17;44 (5) :115605.|Cell Signal. 2025 Jul:131:111709.|Cells. 2024 Apr 19;13 (8) :710.|Eur J Pharmacol. 2025 Sep 15:1003:177942.|Int Immunopharmacol. 2025 Mar 26:150:114278.|Mol Cancer Res. 2019 Oct;17 (10) :2102-2114.|Mol Cancer Ther. 2025 Jun 4;24 (6) :920-930.|Nat Commun. 2019 Aug 2;10 (1) :3485.|Oncogene. 2022 Nov;41 (46) :5020-5031.|Oncogenesis. 2025 Mar 1;14 (1) :4.|Patent. US20210353605A1.|Research Square Preprint. 2021 May.|Research Square Preprint. 2024 Nov 06.|Sci Rep. 2021 Feb 4;11 (1) :3176.|Thorax. 2022 Mar;77 (3) :247-258.|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.|Sci Rep. 2025 Nov 27.

• CAS Number :

  [1234015-52-1]