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Cat. No. Name Size Price Add Cart
KI3385CHIR-124QuoteQuote

Chemical Characteristic

Product NameCHIR-124
CAS No.405168-58-3
Molecular Weight 419.91
FormulaC23H22ClN5O
Chemical Name4-[[(3S)-1-azabicyclo[2.2.2]octan-3-yl]amino]-6-chloro-3-(1,3-dihydrobenzimidazol-2-ylidene)quinolin-2-one
Smiles[nH]1c(=O)c(c(c2cc(ccc12)Cl)N[C@@H]1CN2CCC1CC2)c1nc2c([nH]1)cccc2
Chemical Structure

Biological activities

CHIR-124 is a potent, selective human checkpoint kinase 1 (Chk1) inhibitor. CHIR-124 inhibits Chk1 with an IC50 of 0.3 nM, by occupying the ATP-binding site. CHIR-124 also inhibits Chk2 with an IC50 of 0.7 µM. In vitro, CHIR-124 potently targets other kinases (PDGFR and FLT3) with IC50s of 6.6 and 5.8 nM, respectively. In addition, CHIR-124 sensitizes p53?/? HCT116 cells to ionizing radiation (IR).[1] CHIR-124 interacts synergistically with topoisomerase I poisons in p53-mutant tumor cells. CHIR-124 also abrogates SN38-induced S-phase (by restoring Cdc25A) and G2/M-phase (via Cdc25C hyperphosphorylation) checkpoints, triggering apoptosis. CHIR-124 treatment reverses the suppression of cdc25A by SN-38 in the p53-defective MDA-MB-435 cell line. CHIR-124 alters cellular signaling of Chk1. In vivo, in an orthotopic breast cancer xenograft, CHIR-124 in combination with CPT-11 shows potentiation of tumor growth inhibition and increases apoptosis.[2]

Protocols

In vitro, CHIR-124 is dissolved in DMSO and stored in aliquots at -20 °C.[2]

References

[1] Dai Y, et al. New insights into checkpoint kinase 1 in the DNA damage response signaling network. Clin Cancer Res. 2010, 16(2): 376-383.
[2] Tse AN, et al. CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivo. Clin Cancer Res. 2007, 13(2 Pt 1): 591-602.

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