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CHIR-124

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CHIR-124 Basic information

Product Name:
CHIR-124
Synonyms:
  • CS-2141
  • CHIR-124 (CHIR124
  • CHIR-124
  • 2(1H)-Quinolinone, 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylaMino]-3-(1H-benziMidazol-2-yl)-6-chloro-
  • 4-[((3S)-1-Azabicyclo[2.2.2]oct-3-yl)amino]-3-(1H-benzimidazol-2-yl)-6-chloroquinolin-2(1H)-one
  • CHIR-124 USP/EP/BP
CAS:
405168-58-3
MF:
C23H22ClN5O
MW:
419.91
Product Categories:
  • Inhibitors
Mol File:
405168-58-3.mol
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CHIR-124 Chemical Properties

Density 
1.46
solubility 
insoluble in H2O; ≥10.5 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming
form 
solid
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CHIR-124 Usage And Synthesis

Description

Checkpoint kinase 1 (Chk1) regulates S and G2-M phase cell cycle checkpoints in response to DNA damage. CHIR124 is a cell-permeable, quinolone-based inhibitor of Chk1 (IC50 = 0.3 nM in vitro). It demonstrates high selectivity for Chk1 by displaying inhibitory values 2,000-fold higher against Chk2 (IC50 = 0.7 μM). In synergy with topoisomerase I poisons or ionizing radiation, CHIR124 can inhibit the growth of p53-mutant solid tumor cells both in vitro and in a xenograft model, potentiating tumor apoptosis.

Uses

CHIR 124 is a cell-permeable molecule with a quinolone-based structure. It inhibits checkpoint kinase 1 (Chk1) which regulates S and G2-M cekk cycle checkpoints in response to DNA damage. Application towards inhibition of tumor cell growth.

References

[1]. tse an, rendahl kg, sheikh t, et al. chir-124, a novel potent inhibitor of chk1, potentiates the cytotoxicity of topoisomerase i poisons in vitro and in vivo. clinical cancer research, 2007, 13(2): 591-602.
[2]. tao yg, leteur c, yang cy, et al. radiosensitization by chir-124, a selective chk1 inhibitor effects of p53 and cell cycle checkpoints. cell cycle, 2007, 8(8): 1196-1205.

CHIR-124Supplier

Shanghai Boyle Chemical Co., Ltd.
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Email
sales@boylechem.com
Jinan Trio PharmaTech Co., Ltd.
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+86 (531) 88811783
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sales@trio-pharmatech.com (International market)
Dalian Meilun Biotech Co., Ltd.
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0411-62910999 13889544652
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sales@meilune.com
Hangzhou Sage Chemical Co., Ltd.
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+86057186818502 13588463833
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info@sagechem.com
NCE Biomedical Co.,Ltd.
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4000-027-021 |24 hour enquiry :+86-13986109188 |English:+86-15623472865 |Japanese:+81-08033611988
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CHIR-124(405168-58-3)Related Product Information