For research use only. Not for therapeutic Use.
Prexasertib Mesylate Hydrate（Cat No.:I008873）is a potent and selective inhibitor of checkpoint kinase 1 (CHK1), a key enzyme in the DNA damage response. By inhibiting CHK1, Prexasertib disrupts cell cycle arrest, enhancing DNA damage and promoting apoptosis, particularly in cancer cells with defective DNA repair mechanisms. It is being investigated for its potential in combination therapies for various cancers, including solid tumors and hematologic malignancies. Prexasertib’s ability to sensitize tumors to DNA-damaging treatments makes it a promising candidate in cancer research and drug development.
| Catalog Number | I008873 |
| CAS Number | 1234015-57-6 (mesylate hydrate) |
| Synonyms | LY-2606368; LY2606368; LY 2606368; Prexasertib Mesylate Hydrate.;5-((5-(2-(3-aminopropoxy)-6-methoxyphenyl)-1H-pyrazol-3-yl)amino)pyrazine-2-carbonitrile methanesulfonate hydrate |
| Molecular Formula | C19H25N7O6S |
| Purity | ≥95% |
| Target | Chk1 inhibitor |
| Solubility | Soluble in DMSO |
| Storage | 0 - 4 °C for short term, or -20 °C for long term |
| IUPAC Name | 5-[[5-[2-(3-aminopropoxy)-6-methoxyphenyl]-1H-pyrazol-3-yl]amino]pyrazine-2-carbonitrile;methanesulfonic acid;hydrate |
| InChI | InChI=1S/C18H19N7O2.CH4O3S.H2O/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);1H2 |
| InChIKey | LCYWXOLNJNHLGN-UHFFFAOYSA-N |
| SMILES | COC1=C(C(=CC=C1)OCCCN)C2=CC(=NN2)NC3=NC=C(N=C3)C#N.CS(=O)(=O)O.O |
| Reference | </br> 1: 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 Mar 7. pii: clincanres.2876.2016. doi: 10.1158/1078-0432.CCR-16-2876. [Epub ahead of print] PubMed PMID: 28270495.</br> 2: 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 Jan 30. pii: molcanther.0352.2016. doi: 10.1158/1535-7163.MCT-16-0352. [Epub ahead of print] PubMed PMID: 28138028.</br> 3: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. |
