WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 406341
CAS#: 405168-58-3
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.
MedKoo Cat#: 406341
Name: CHIR-124
CAS#: 405168-58-3
Chemical Formula: C23H22ClN5O
Exact Mass: 419.15129
Molecular Weight: 419.91
Elemental 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
Appearance: Solid powder
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
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.
