CHIR-124
Cat. No.:YN440257
产品名称: | CHIR-124 |
CAS No.: | 405168-58-3 |
Chemical Name: | 4-[(3S)-1-azabicyclo[2.2.2]oct-3-ylamino]-3-(1H-benzimidazol-2-yl)-6-chloro-2(1H)-quinolinone |
Synonyms: | CHIR 124,CHIR124 |
分子量: | 419.91 |
分子式: | C₂₃H₂₂ClN₅O |
SMILES: | ClC1=CC2=C(NC(C(C3=NC4=C(C=CC=C4)N3)=C2N[C@@H]5CN6CCC5CC6)=O)C=C1 |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | CHIR-124 是一种有效的,选择性的Chk1抑制剂,IC50值为 0.3 nM;同时可有效抑制PDGFR和FLT3,IC50值分别为 6.6 nM 和 5.8 nM。 |
IC50和靶点: | [{name:"Chk1:0.3 nM (IC50)"},{name: "Chk2:697.4 nM (IC50)"},{name: "PDGFR:6.6 nM (IC50)"},{name: "FLT3:5.8 nM (IC50)"},{name: "Cdk4/cyclin D:2.05 μM (IC50)"},{name: "CDC2/cyclin B:0.5057 μM (IC50)"},{name: "Cdk2/cyclin A:0.1911 μM (IC50)"},{name: "bFGFR:2.01 μM (IC50)"},{name: "FGFR3:1.29 μM (IC50)"},{name: "VEGFR2 FLK1:0.5779 μM (IC50)"},{name: "VEGFR1 FLT1:0.4636 μM (IC50)"},{name: "PKCα:0.58 μM (IC50)"},{name: "PKAβ I:2.25 μM (IC50)"},{name: "PKCβ II:0.58 μM (IC50)"},{name: "PKCγ:0.11 μM (IC50)"},{name: "ERK2:4.31 μM (IC50)"},{name: "PKA:0.1031 μM (IC50)"},{name: "GSK3:0.0233 μM (IC50)"}] |
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Tse, A.N., Rendahl, K.G., Sheikh, T., et al.CHIR-124, a novel potent inhibitor of Chk1, potentiates the cytotoxicity of topoisomerase I poisons in vitro and in vivoClin. Cancer Res.13(2 Pt 1),591-602(2007)
Tao, Y., Leteur, C., Yang, C., et al.Radiosensitization by Chir-124, a selective CHK1 inhibitor: Effects of p53 and cell cycle checkpointsCell Cycle8(8),1196-1205(2009)