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Prexasertib (dihydrochloride)

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].

Product Specifications

CAS Number

[1234015-54-3]

Product Name Alternative

LY2606368 (dihydrochloride)

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-dihydrochloride.html

Purity

99.73

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 Formula

C18H21Cl2N7O2

Molecular Weight

438.31

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

4°C (Powder, sealed storage, away from moisture)

Scientific Category

Reference compound1

Clinical Information

Phase 2

Isoform

Chk1; Chk2

Citation 01

BioRxiv. September 10, 2021.|Methods Mol Biol. 2018:1711:351-398.|Neurooncol Adv. 2024 Nov 19;6 (1) :vdae187.|Sci Rep. 2025 Nov 27.|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.

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