Prexasertib mesylate
Based on 37 publication(s) in Google Scholar
Prexasertib mesylate (LY2606368 mesylate) 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 mesylate inhibits CHK2 (IC50=8 nM) and RSK1 (IC50=9 nM). Prexasertib mesylate causes double-stranded DNA breakage and replication catastrophe resulting in apoptosis. Prexasertib mesylate shows potent anti-tumor activity.
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- CAS. Nr.: 1234015-55-4
- Formel: C19H23N7O5S
- Molecular Weight:461.49
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Publications Citing Use of MedChemExpress (MCE) Prexasertib mesylate
More- Nat Commun. 2019 Aug 2;10(1):3485. [Abstract]
- Sci Adv. 2026 Jun 26;12(26):eadz3351. [Abstract]
- Cell Death Dis. 2026 Mar 26;17(1):375. [Abstract]
- Cancer Lett. 2026 Feb 4;642:218300.
- Cancer Lett. 2026 Apr 1:642:218300. [Abstract]
- Oncogene. 2026 Jun 10. [Abstract]
- Oncogene. 2022 Nov;41(46):5020-5031. [Abstract]
- Thorax. 2022 Mar;77(3):247-258. [Abstract]
- Cell Chem Biol. 2026 Jun 18;33(6):767-784.e7. [Abstract]
- Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
- Cell Rep. 2025 Apr 17;44(5):115605. [Abstract]
- Mol Cancer Ther. 2025 Jun 4;24(6):920-930. [Abstract]
- Oncogenesis. 2025 Mar 1;14(1):4. [Abstract]
- Cells. 2024 Apr 19;13(8):710. [Abstract]
- Mol Cancer Res. 2019 Oct;17(10):2102-2114. [Abstract]
- Eur J Pharmacol. 2025 Sep 15:1003:177942. [Abstract]
- Cell Biol Toxicol. 2023 Jun;39(3):795-811. [Abstract]
- Int Immunopharmacol. 2026 Feb 15:171:116126. [Abstract]
- Int Immunopharmacol. 2025 Mar 26:150:114278. [Abstract]
- Sci Rep. 2025 Nov 27. [Abstract]
- Sci Rep. 2021 Feb 4;11(1):3176. [Abstract]
- Cancers (Basel). 2021 Aug 20;13(16):4200. [Abstract]
- Cancers (Basel). 2020 Aug 26;12(9):2426. [Abstract]
- Cancers (Basel). 2020 Jun 29;12(7):1726. [Abstract]
- Cell Signal. 2025 Jul:131:111709. [Abstract]
- Neurooncol Adv. 2024 Nov 19;6(1):vdae187. [Abstract]
- bioRxiv. 2025 Dec 25.
- bioRxiv. 2025 April 17.
- Research Square Preprint. 2024 Nov 06.
- bioRxiv. 2024 Nov 6:2024.11.04.621884. [Abstract]
- Universität Hamburg. 2022 Aug.
- Utrecht University. 2023 Feb.
- bioRxiv. January 04, 2022.
- Patent. US20210353605A1.
- bioRxiv. September 10, 2021.
- Research Square Preprint. 2021 May.
- Methods Mol Biol. 2018:1711:351-398. [Abstract]
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Biologische Aktivität
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Chk1 0.9 nM (Ki) |
Chk1 <1 nM (IC50) |
Chk2 8 nM (IC50) |
Prexasertib (LY2606368) mesylate inhibits MELK (IC50=38 nM), SIK (IC50=42 nM), BRSK2 (IC50=48 nM), ARK5 (IC50=64 nM). Prexasertib mesylate requires CDC25A and CDK2 to cause DNA damage[1].
Prexasertib mesylate (33, 100 nM; for 7 hours) results in DNA damage during S-phase in HeLa cells[1].
Prexasertib mesylate (8-250 nM; pre-treated for 15 minutes) inhibits CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) in HT-29 cells[1].
Prexasertib mesylate (4 nM; 24 hours) results in a large shift in cell-cycle populations from G1 and G2-M to S-phase with an accompanied induction of H2AX phosphorylation in U-2 OS cells[1].
Prexasertib mesylate (33 nM; for 12 hours) causes chromosomal fragmentation in HeLa cells. Prexasertib mesylate (100 nM; 0.5 to 9 hours) induces replication stress and depletes the pool of available RPA2 for binding to DNA[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HeLa cells
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Concentration:33, 100 nM
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Incubation Time:7 hours
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Result:Had an IC50 of 37 nM and resulted in the G2-M population received DNA damage during S-phase but continued to progress through the cell cycle into an early mitosis.
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Cell Line:HT-29 cells
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Concentration:8, 16, 31, 63, 125, 250 nM
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Incubation Time:Pre-treated for 15 minutes
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Result:Inhibited CHK1 autophosphorylation (S296) and CHK2 autophosphorylation (S516) (IC50 of less than 31 nM) in HT-29 cells.
Prexasertib mesylate (15 mg/kg; SC) causes CHK1 inhibition in the blood and the phosphorylation of both H2AX (S139) and RPA2 (S4/S8)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female CD-1 nu-/nu- mice (26-28 g) with Calu-6 cells[1]
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Dosage:1, 3.3, or 10 mg/kg
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Administration:SC; twice daily for 3 days, rest 4 days; for three cycles
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Result:Caused statistically significant tumor growth inhibition (up to 72.3%).
Chemical Information
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CAS. Nr. 1234015-55-4
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Molecular Weight 461.49
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Formel C19H23N7O5S
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SMILES
N#CC1=NC=C(NC2=NNC(C3=C(OC)C=CC=C3OCCCN)=C2)N=C1.CS(=O)(O)=O
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Synonyms
LY2606368 mesylate
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Publications (37)
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Journal Impact Factor
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Most Recent
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Nat Commun
MYC paralog-dependent apoptotic priming orchestrates a spectrum of vulnerabilities in small cell lung cancer. [Abstract]2019 Aug 2;10(1):3485. PMID: 31375684
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Nat Commun. 2019 Aug 2;10(1):3485. [Abstract]
Viability of mock control and Myc-activated CRISPRa cells upon treatment with 40 nM prexasertib for 96 h (n = 3).
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Sci Adv
Patient-derived organoids across cancers reveal conserved tumor heterogeneity and actionable therapeutic vulnerabilities. [Abstract]2026 Jun 26;12(26):eadz3351. PMID: 42361179 -
Cell Death Dis
2026 Mar 26;17(1):375. PMID: 41888112 -
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Cancer Lett
2026 Apr 1:642:218300. PMID: 41651400 -
Oncogene
DNA replication stress and translational repression converge to drive CDK1- and caspase-dependent apoptosis in Ewing sarcoma. [Abstract]2026 Jun 10. PMID: 42270776 -
Oncogene
Distinct roles of treatment schemes and BRCA2 on the restoration of homologous recombination DNA repair and PARP inhibitor resistance in ovarian cancer. [Abstract]2022 Nov;41(46):5020-5031. PMID: 36224341 -
Thorax
Potential for inhibition of checkpoint kinases 1/2 in pulmonary fibrosis and secondary pulmonary hypertension. [Abstract]2022 Mar;77(3):247-258. PMID: 34226205 -
Cell Chem Biol
The cytotoxic effect of prexasertib is a consequence of dual inhibition on both CHK1 and AMPK. [Abstract]2026 Jun 18;33(6):767-784.e7. PMID: 42061410 -
Br J Cancer
Interferon regulatory factor 1 (IRF-1) downregulates Checkpoint kinase 1 (CHK1) through miR-195 to upregulate apoptosis and PD-L1 expression in Hepatocellular carcinoma (HCC) cells. [Abstract]2021 Jul;125(1):101-111. PMID: 33772151
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Full length and cleaved PARP protein expressions are determined by western blot in Hepa1-6 cells and Huh-7 cells induced by prexasertib with dose of 1 µM and 5 nM for 24 h, respectively.
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Representative image of FACS analysis of late apoptotic Hepa1-6 cell rate treated by DMSO or prexasertib with dose of 1 µM for 24 h are shown.
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Tumour growth curves (Mean ± SEM) of murine HCC model treated by vehicle (n = 8) or prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8) are shown.
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days). Representative images of TUNEL assay for cellular apoptosis (green staining) in tumours are shown.
Prexasertib mesylate purchased from MedChemExpress. Usage Cited in: Br J Cancer. 2021 Jul;125(1):101-111. [Abstract]
Prexasertib (10mg/kg, subcutaneous injection, 2 of 7 days, n = 8). PD-L1 mRNA expression is determined by qPCR in tumours treated by prexasertib or vehicle.
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Cell Rep
The low-dose CHK1 inhibitor prexasertib triggers VDAC1 dephosphorylation to activate mtDNA-STING signaling and synergize immunotherapy. [Abstract]2025 Apr 17;44(5):115605. PMID: 40249707 -
Mol Cancer Ther
Targeting Monounsaturated Fatty Acid Metabolism for Radiosensitization of KRAS Mutant 3D Lung Cancer Models. [Abstract]2025 Jun 4;24(6):920-930. PMID: 39834305 -
Oncogenesis
STAG2 expression imparts distinct therapeutic vulnerabilities in muscle-invasive bladder cancer cells. [Abstract]2025 Mar 1;14(1):4. PMID: 40025053 -
Cells
Genomic Engineering of Oral Keratinocytes to Establish In Vitro Oral Potentially Malignant Disease Models as a Platform for Treatment Investigation. [Abstract]2024 Apr 19;13(8):710. PMID: 38667326 -
Mol Cancer Res
Pharmacologic Ascorbate Primes Pancreatic Cancer Cells for Death by Rewiring Cellular Energetics and Inducing DNA Damage. [Abstract]2019 Oct;17(10):2102-2114. PMID: 31337671 -
Eur J Pharmacol
VOPP1, a determinant of the sensitivity of non-small cell lung cancer cells to NAE inhibitors. [Abstract]2025 Sep 15:1003:177942. PMID: 40651787 -
Cell Biol Toxicol
Exploring the ATR-CHK1 pathway in the response of doxorubicin-induced DNA damages in acute lymphoblastic leukemia cells. [Abstract]2023 Jun;39(3):795-811. PMID: 34519926 -
Int Immunopharmacol
CHK1 inhibition by prexasertib sensitizes cisplatin-resistant malignant tumor cells via checkpoint abrogation and STAT1-driven PD-L1 upregulation. [Abstract]2026 Feb 15:171:116126. PMID: 41477994 -
Int Immunopharmacol
Prexasertib exerts a synergistic effect on the antitumor activity of Lenvatinib through ALOX15-mediated ferroptosis in hepatocellular carcinoma. [Abstract]2025 Mar 26:150:114278. PMID: 39954659 -
Sci Rep
Synergistic inhibition of CHK1 and MUS81 to combat replication stress resistance in high-risk neuroblastoma. [Abstract]2025 Nov 27. PMID: 41310217 -
Sci Rep
The mitotic checkpoint is a targetable vulnerability of carboplatin-resistant triple negative breast cancers. [Abstract]2021 Feb 4;11(1):3176. PMID: 33542435 -
Cancers (Basel)
Novel Insights into the Molecular Regulation of Ribonucleotide Reductase in Adrenocortical Carcinoma Treatment. [Abstract]2021 Aug 20;13(16):4200. PMID: 34439352 -
Cancers (Basel)
Systems Biology Approach Identifies Prognostic Signatures of Poor Overall Survival and Guides the Prioritization of Novel BET-CHK1 Combination Therapy for Osteosarcoma. [Abstract]2020 Aug 26;12(9):2426. PMID: 32859084 -
Cancers (Basel)
Cotargeting CHK1 and PI3K Synergistically Suppresses Tumor Growth of Oral Cavity Squamous Cell Carcinoma in Patient-Derived Xenografts. [Abstract]2020 Jun 29;12(7):1726. PMID: 32610557 -
Cell Signal
2025 Jul:131:111709. PMID: 40037423 -
Neurooncol Adv
Ion channel modulator DPI-201-106 significantly enhances antitumor activity of DNA damage response inhibitors in glioblastoma. [Abstract]2024 Nov 19;6(1):vdae187. PMID: 39659830 -
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bioRxiv
PAIRWISE: Deep Learning-based Prediction of Effective Personalized Drug Combinations in Cancer. [Abstract]2024 Nov 6:2024.11.04.621884. PMID: 39574568 -
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Methods Mol Biol
2018:1711:351-398. PMID: 29344898
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
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Prexasertib mesylate Related Classifications
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