| Identification | Back Directory | [Name]
CHIR-124 | [CAS]
405168-58-3 | [Synonyms]
CS-2141
CHIR-124
CHIR-124
(CHIR124
CHIR-124 USP/EP/BP
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 | [Molecular Formula]
C23H22ClN5O | [MDL Number]
MFCD14636453 | [MOL File]
405168-58-3.mol | [Molecular Weight]
419.91 |
| Chemical Properties | Back Directory | [density ]
1.46 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in H2O; ≥10.5 mg/mL in DMSO; ≥2.61 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
9.00±0.70(Predicted) | [color ]
Light yellow to brown |
| Hazard Information | Back Directory | [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. | [storage]
Store at -20°C | [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. |
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NCE Biomedical Co.,Ltd.
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