CHIR-124

featured

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

Description:CHIR-124 is a quinolone-based small molecule Chk1 inhibitor, that is structurally unrelated to other known inhibitors of Chk1. It potently and selectively inhibits Chk1 in vitro (IC(50) = 0.0003 micromol/L). CHIR-124 interacts synergistically with topoisomerase poisons (e.g., camptothecin or SN-38) in causing growth inhibition in several p53-mutant solid tumor cell lines as determined by isobologram or response surface analysis. CHIR-124 is a novel and potent Chk1 inhibitor with promising antitumor activities when used in combination with topoisomerase I poisons.

Price and Availability

CHIR-124 purity > 98%, is in stock. Current shipping out time is about 2 weeks after order is received. CoA, QC data and MSDS documents are available in one week after order is received.

Chemical Structure

Theoretical Analysis

MedKoo Cat#: 406341Name: CHIR-124CAS#: 405168-58-3Chemical Formula: C23H22ClN5OExact Mass: 419.15129Molecular Weight: 419.91Elemental Analysis: C, 65.79; H, 5.28; Cl, 8.44; N, 16.68; O, 3.81

Synonym:CHIR124; CHIR-124; CHIR 124.

IUPAC/Chemical Name:3-(1H-benzo[d]imidazol-2-yl)-6-chloro-4-((1R,3S,4R)-quinuclidin-3-ylamino)quinolin-2(1H)-one.

InChi Key:MOVBBVMDHIRCTG-LJQANCHMSA-N

InChi Code:InChI=1S/C23H22ClN5O/c24-14-5-6-16-15(11-14)21(25-19-12-29-9-7-13(19)8-10-29)20(23(30)28-16)22-26-17-3-1-2-4-18(17)27-22/h1-6,11,13,19H,7-10,12H2,(H,26,27)(H2,25,28,30)/t19-/m1/s1

SMILES Code:O=C1NC2=C(C=C(Cl)C=C2)C(N[C@@H]3C[N@]4CC[C@]3([H])CC4)=C1C5=NC6=CC=CC=C6N5

Technical Data

Additional Information

References

1: Dufau I, Frongia C, Sicard F, Dedieu L, CordelierP, Ausseil F, Ducommun B, Valette A. Multicellular tumor spheroid modelto evaluate spatio-temporal dynamics effect of chemotherapeutics:application to the gemcitabine/CHK1 inhibitor combination in pancreaticcancer. BMC Cancer. 2012 Jan 13;12:15. doi: 10.1186/1471-2407-12-15.PubMed PMID: 22244109; PubMed Central PMCID: PMC3280152.

2: Lee JH, Choy ML, Ngo L, Venta-Perez G, Marks PA. Role of checkpointkinase 1 (Chk1) in the mechanisms of resistance to histone deacetylaseinhibitors. Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19629-34. doi:10.1073/pnas.1117544108. Epub 2011 Nov 21. PubMed PMID: 22106282; PubMedCentral PMCID: PMC3241758.

3: Tao Y, Leteur C, Yang C, Zhang P, Castedo M, Pierré A, Golsteyn RM,Bourhis J, Kroemer G, Deutsch E. Radiosensitization by Chir-124, aselective CHK1 inhibitor: effects of p53 and cell cycle checkpoints.Cell Cycle. 2009 Apr 15;8(8):1196-205. Epub 2009 Apr 16. PubMed PMID:19305158.

4: Seiler JA, Conti C, Syed A, Aladjem MI, Pommier Y. The intra-S-phasecheckpoint affects both DNA replication initiation and elongation:single-cell and -DNA fiber analyses. Mol Cell Biol. 2007Aug;27(16):5806-18. Epub 2007 May 21. PubMed PMID: 17515603; PubMedCentral PMCID: PMC1952133.

5: Tse AN, Rendahl KG, Sheikh T, Cheema H, Aardalen K, Embry M, Ma S,Moler EJ, Ni ZJ, Lopes de Menezes DE, Hibner B, Gesner TG, Schwartz GK.CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicityof topoisomerase I poisons in vitro and in vivo. Clin Cancer Res. 2007Jan 15;13(2 Pt 1):591-602. PubMed PMID: 17255282.