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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 | | EINECS: | | Product Categories: | Inhibitors | | Mol File: | 405168-58-3.mol |
| 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 |
| 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-124 Preparation Products And Raw materials |
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