Prexasertib mesylate

    WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 206787

CAS#: 1234015-55-4 (mesylate)

Description: Prexasertib, also known as LY2606368, is a potent and selective Chk1/Chk2 inhibitor. Prexasertib increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Treatment of cells with LY2606368 results in the rapid appearance of TUNEL and pH2AX-positive double-stranded DNA breaks in the S-phase cell population.

Price and Availability


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Prexasertib mesylate, purity > 98%, is in stock. The same day shipping out after order is received. Note: the estimated shipping out time for order > 200mg may be 2 weeks.

Chemical Structure


Theoretical Analysis

MedKoo Cat#: 206787
Name: Prexasertib mesylate
CAS#: 1234015-55-4 (mesylate)
Chemical Formula: C19H23N7O5S
Exact Mass:
Molecular Weight: 461.497
Elemental Analysis: C, 49.45; H, 5.02; N, 21.25; O, 17.33; S, 6.95

Related CAS #: 1234015-54-3 (2HCl)   1234015-55-4 (mesylate)   1234015-52-1 (free base)   1234015-57-6 (mesylate hydrate)    

Synonym: Prexasertib mesylate; LY2606368; LY-2606368; LY 2606368.

IUPAC/Chemical Name: 2-Pyrazinecarbonitrile, 5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)-, methanesulfonate


InChi Code: InChI=1S/C18H19N7O2.CH4O3S/c1-26-14-4-2-5-15(27-7-3-6-19)18(14)13-8-16(25-24-13)23-17-11-21-12(9-20)10-22-17;1-5(2,3)4/h2,4-5,8,10-11H,3,6-7,19H2,1H3,(H2,22,23,24,25);1H3,(H,2,3,4)


Technical Data

Yellow solid powder

>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:

Safety Data Sheet (MSDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Soluble in DMSO

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

Harmonized System Code:


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3: Zhong B, Maharaj A, Davis A, Roussel MF, Stewart CF. Development and validation of a sensitive LC MS/MS method for the measurement of the checkpoint kinase 1 inhibitor prexasertib and its application in a cerebral microdialysis study. J Pharm Biomed Anal. 2018 Jul 15;156:97-103. doi: 10.1016/j.jpba.2018.04.018. Epub 2018 Apr 17. PubMed PMID: 29698863; PubMed Central PMCID: PMC5984718.

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7: Brill E, Yokoyama T, Nair J, Yu M, Ahn YR, Lee JM. Prexasertib, a cell cycle checkpoint kinases 1 and 2 inhibitor, increases in vitro toxicity of PARP inhibition by preventing Rad51 foci formation in BRCA wild type high-grade serous ovarian cancer. Oncotarget. 2017 Oct 31;8(67):111026-111040. doi: 10.18632/oncotarget.22195. eCollection 2017 Dec 19. PubMed PMID: 29340034; PubMed Central PMCID: PMC5762302.

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9: Sen T, Tong P, Stewart CA, Cristea S, Valliani A, Shames DS, Redwood AB, Fan YH, Li L, Glisson BS, Minna JD, Sage J, Gibbons DL, Piwnica-Worms H, Heymach JV, Wang J, Byers LA. CHK1 Inhibition in Small-Cell Lung Cancer Produces Single-Agent Activity in Biomarker-Defined Disease Subsets and Combination Activity with Cisplatin or Olaparib. Cancer Res. 2017 Jul 15;77(14):3870-3884. doi: 10.1158/0008-5472.CAN-16-3409. Epub 2017 May 10. PubMed PMID: 28490518; PubMed Central PMCID: PMC5563854.

10: Manic G, Signore M, Sistigu A, Russo G, Corradi F, Siteni S, Musella M, Vitale S, De Angelis ML, Pallocca M, Amoreo CA, Sperati F, Di Franco S, Barresi S, Policicchio E, De Luca G, De Nicola F, Mottolese M, Zeuner A, Fanciulli M, Stassi G, Maugeri-Saccà M, Baiocchi M, Tartaglia M, Vitale I, De Maria R. CHK1-targeted therapy to deplete DNA replication-stressed, p53-deficient, hyperdiploid colorectal cancer stem cells. Gut. 2018 May;67(5):903-917. doi: 10.1136/gutjnl-2016-312623. Epub 2017 Apr 7. PubMed PMID: 28389531; PubMed Central PMCID: PMC5890648.

11: Lowery CD, VanWye AB, Dowless M, Blosser W, Falcon BL, Stewart J, Stephens J, Beckmann RP, Bence Lin A, Stancato LF. The Checkpoint Kinase 1 Inhibitor Prexasertib Induces Regression of Preclinical Models of Human Neuroblastoma. Clin Cancer Res. 2017 Aug 1;23(15):4354-4363. doi: 10.1158/1078-0432.CCR-16-2876. Epub 2017 Mar 7. PubMed PMID: 28270495.

12: Zeng L, Beggs RR, Cooper TS, Weaver AN, Yang ES. Combining Chk1/2 Inhibition with Cetuximab and Radiation Enhances In Vitro and In Vivo Cytotoxicity in Head and Neck Squamous Cell Carcinoma. Mol Cancer Ther. 2017 Apr;16(4):591-600. doi: 10.1158/1535-7163.MCT-16-0352. Epub 2017 Jan 30. PubMed PMID: 28138028; PubMed Central PMCID: PMC5560482.

13: Ghelli Luserna Di Rorà A, Iacobucci I, Imbrogno E, Papayannidis C, Derenzini E, Ferrari A, Guadagnuolo V, Robustelli V, Parisi S, Sartor C, Abbenante MC, Paolini S, Martinelli G. Prexasertib, a Chk1/Chk2 inhibitor, increases the effectiveness of conventional therapy in B-/T- cell progenitor acute lymphoblastic leukemia. Oncotarget. 2016 Aug 16;7(33):53377-53391. doi: 10.18632/oncotarget.10535. PubMed PMID: 27438145; PubMed Central PMCID: PMC5288194.

14: Hong D, Infante J, Janku F, Jones S, Nguyen LM, Burris H, Naing A, Bauer TM, Piha-Paul S, Johnson FM, Kurzrock R, Golden L, Hynes S, Lin J, Lin AB, Bendell J. Phase I Study of LY2606368, a Checkpoint Kinase 1 Inhibitor, in Patients With Advanced Cancer. J Clin Oncol. 2016 May 20;34(15):1764-71. doi: 10.1200/JCO.2015.64.5788. Epub 2016 Apr 4. PubMed PMID: 27044938; PubMed Central PMCID: PMC5321045.

15: King C, Diaz HB, McNeely S, Barnard D, Dempsey J, Blosser W, Beckmann R, Barda D, Marshall MS. LY2606368 Causes Replication Catastrophe and Antitumor Effects through CHK1-Dependent Mechanisms. Mol Cancer Ther. 2015 Sep;14(9):2004-13. doi: 10.1158/1535-7163.MCT-14-1037. Epub 2015 Jul 3. PubMed PMID: 26141948.