CHIR-124

• CAT Number: I003475
• CAS Number: 405168-58-3
• Molecular Formula: C23H22ClN5O
• Molecular Weight: 419.9
• Purity: ≥95%
• Target: Chk
• Solubility: DMSO: ≥ 14 mg/mL
• Storage: 3 years -20℃ powder
• IUPAC Name: 4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-3-(1H-benzimidazol-2-yl)-6-chloro-1H-quinolin-2-one
• InChI: 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
• InChIKey: MOVBBVMDHIRCTG-LJQANCHMSA-N
• SMILES: C1CN2CCC1[C@@H](C2)NC3=C(C(=O)NC4=C3C=C(C=C4)Cl)C5=NC6=CC=CC=C6N5

CHIR-124 (Cat.No:I003475) is a novel and potent chk1 inhibitor with an IC50 of 0.3 nM. Chk1 kinase is a critical regulator of both the S and G2/M phase cell cycle checkpoints in response to DNA damage. CHIR-124 has been shown that inhibitors of chk1 can selectively sensitize tumor cells with mutant p53 to genotoxic agents.

Reference

1:Radiosensitization by Chir-124, a selective CHK1 inhibitor: effects of p53 and cell cycle checkpoints. Tao Y, Leteur C, Yang C, Zhang P, Castedo M, Pierré A, Golsteyn RM, Bourhis J, Kroemer G, Deutsch E.Cell Cycle. 2009 Apr 15;8(8):1196-205. Epub 2009 Apr 16. PMID: 19305158 2:CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. 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.Clin Cancer Res. 2007 Jan 15;13(2 Pt 1):591-602. PMID: 17255282 Free Article