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编 号：F763031
分子式：C21H18ClFN2O3
分子量：400.83
分子式：C21H18ClFN2O3
分子量：400.83
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CAS No: 3031418-84-2
产品详情
生物活性：
Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
体内研究：
Topo I/COX-2-IN-1 (1H-30) (intraperitoneal injection, 100 mg/kg, twice a day, 14 days) may inhibit tumor growth by increasing the expression of caspase-3 and decreasing MMP-9 and COX-2 in tumor tissues to induce apoptosis in BALB/c mice model infected with CT26.WT colon cancer cells.Animal Model:BALB/c mice model infected with CT26.WT colon cancer cells
Dosage:100 mg/kg
Administration:Intraperitoneal injection; twice a day; 14 days
Result:Significant reduction in tumor size and tumor weight and no significant differences in body weight, organs.
Animal Model:SD rats
Dosage:100 mg/kg
Administration:Intraperitoneal injection; once
Result:b>The pharmacokinetic parameters of Topo I/COX-2-IN-1 (1H-30) ParameterTopo I/COX-2-IN-1 (1H-30)
t1/21.56 h
Tmax0.67 h
Cmax20.19 μg/mL
AUC0-t18.20 mg/L?h
AUC0?inf_obs18.60 mg/L?h
体外研究：
Topo I/COX-2-IN-1 (1H-30) (0-100 μM, 24 h) has anti-tumor cell proliferation activity and can induce apoptosis by increasing caspase-3 activity in a dose-dependent manner.Topo I/COX-2-IN-1 (1H-30) (0.04-0.37 μM, 48 h) shows a significant decrease in cell migration at 0.37 μM and reduces the expression of MMP-9 (matrix metalloproteinases) in HGC-27 and RKO cells.Topo I/COX-2-IN-1 (1H-30) (10 μM, 48 h) can inhibit the activation of NF-κB pathway in cancer cells.
Topo I/COX-2-IN-1 (1H-30) is a potential Topo I/COX-2 inhibitor. Topo I/COX-2-IN-1 inhibits COX-2 and Topo I with the IC50 value of 0.24 μM and 4.42 μM, respectively. Topo I/COX-2-IN-1 can induce apoptosis and inhibit migration of cancer cells, has anti-cancer activity.
体内研究：
Topo I/COX-2-IN-1 (1H-30) (intraperitoneal injection, 100 mg/kg, twice a day, 14 days) may inhibit tumor growth by increasing the expression of caspase-3 and decreasing MMP-9 and COX-2 in tumor tissues to induce apoptosis in BALB/c mice model infected with CT26.WT colon cancer cells.Animal Model:BALB/c mice model infected with CT26.WT colon cancer cells
Dosage:100 mg/kg
Administration:Intraperitoneal injection; twice a day; 14 days
Result:Significant reduction in tumor size and tumor weight and no significant differences in body weight, organs.
Animal Model:SD rats
Dosage:100 mg/kg
Administration:Intraperitoneal injection; once
Result:b>The pharmacokinetic parameters of Topo I/COX-2-IN-1 (1H-30) ParameterTopo I/COX-2-IN-1 (1H-30)
t1/21.56 h
Tmax0.67 h
Cmax20.19 μg/mL
AUC0-t18.20 mg/L?h
AUC0?inf_obs18.60 mg/L?h
体外研究：
Topo I/COX-2-IN-1 (1H-30) (0-100 μM, 24 h) has anti-tumor cell proliferation activity and can induce apoptosis by increasing caspase-3 activity in a dose-dependent manner.Topo I/COX-2-IN-1 (1H-30) (0.04-0.37 μM, 48 h) shows a significant decrease in cell migration at 0.37 μM and reduces the expression of MMP-9 (matrix metalloproteinases) in HGC-27 and RKO cells.Topo I/COX-2-IN-1 (1H-30) (10 μM, 48 h) can inhibit the activation of NF-κB pathway in cancer cells.
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