CHIR-124

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Chemical Information

Product name：CHIR-124	Purity：98% min
CAS NO：405168-58-3	Solubility：DMSO : 14 mg/mL (33.34 mM)
Molecular Formula：C₂₃H₂₂ClN₅O	Package：Package according to customer requirements
Molecular Weight：419.907	Storage：Store at -20℃

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Remarks

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.

Related Prodcuts:

Fidaxomicin; Marbofloxacin; CP-466722; TTP 22; D-64131; M344; Reversine; Pralatrexate; XL228; VE-822; RI-1; SRPIN340; XL888; Rigosertib; APY29; NMS-873; PF-03758309; Telatinib

References

[1]. 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.

[2]. 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.