Synonym
CHIR124; CHIR-124; CHIR 124.
IUPAC/Chemical Name
(S)-3-(1H-Benzo[d]imidazol-2-yl)-6-chloro-4-(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]3CN4CCC3CC4)=C1C5=NC6=CC=CC=C6N5
Purity
>98% (or refer to the Certificate of Analysis)
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).
Solubility
Soluble in DMSO, not soluble in water.
Shelf Life
>2 years if stored properly.
Drug Formulation
CHIR-124 may be formulated in DMSO.
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
Preparing Stock Solutions
The following data is based on the
product
molecular weight
419.91
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
| 1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
| 5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
| 10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
| 50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
1: Dufau I, Frongia C, Sicard F, Dedieu L, Cordelier P, Ausseil F, Ducommun B, Valette A. Multicellular tumor spheroid model to evaluate spatio-temporal dynamics effect of chemotherapeutics: application to the gemcitabine/CHK1 inhibitor combination in pancreatic cancer. 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 checkpoint kinase 1 (Chk1) in the mechanisms of resistance to histone deacetylase inhibitors. 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; PubMed Central 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, a selective 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-phase checkpoint affects both DNA replication initiation and elongation: single-cell and -DNA fiber analyses. Mol Cell Biol. 2007 Aug;27(16):5806-18. Epub 2007 May 21. PubMed PMID: 17515603; PubMed Central 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 cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602. PubMed PMID: 17255282.
