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编 号：F763000
分子式：C27H21N5O6
分子量：511.49
分子式：C27H21N5O6
分子量：511.49
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CAS No: 3031403-77-4
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生物活性：
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
体内研究：
Topoisomerase I/II inhibitor 4 (compound F16) (10-50 mg/kg; i.v.; per 2 days, for 7 days) suppresses tumor growth in the A375 Xenograft Model.Topoisomerase I/II inhibitor 4 (compound F16) of the plasma clearance rate (CL) was 7-fold lower than that of VP-16(0.007 L/min/kg). Topoisomerase I/II inhibitor 4 has a delayed elimination half-life of 151 min.Animal Model:Female BALB/c nude mice (5?6 weeks)
Dosage:10 and 20 mg/kg
Administration:Intravenous injection; Per 2 days, for 14 days.
Result:Inhibited tumor growth in a melanoma xenograft mouse model and no apparent loss in body weight.
Animal Model:Kunming male mice
Dosage:10 mg/kg
Administration:Intravenous injection; for 5 , 15 , 30 , 60 , 120 , 240 and 360 min.
Result:1.19ParameterF16VP-16
Dose (i.v.) mg/kg1010
Cmax (ng/mL)2695217712
Tmax (min)55
AUCplasma (min*ng/mL)2878363409528
T1/2 (min)15145
Vd (L/Kg)0.23410.432
CL (L/min/kg)0.0010.007
体外研究：
Topoisomerase I/II inhibitor 4 (compound F16) (0-100 μM) could intercalate into DNA to inhibit enzymatic activity and inhibit Topo I and II activities in a dose-dependent manner.Topoisomerase I/II inhibitor 4 (compound F16) shows a high-expression level of Topo I and II enzymes in A375 and HCT116 cells and exhibits potent anti-proliferative activity with IC50 values of 20 and 50 nM, respectively, 10-fold lower than L02.Topoisomerase I/II inhibitor 4 (compound F16) (0-40 nM, A375 cell) inhibits cancer cell colony formation, invasion, migration and induces cell apoptosis.
Topoisomerase I/II inhibitor 4 (compound F16) is a potent topoisomerase I (Topo I) and II (Topo II) dual inhibitor. Topoisomerase I/II inhibitor 4 inhibits cell proliferation, invasion and migration and induces apoptosis. Topoisomerase I/II inhibitor 4 can be used for liver cancer research.
体内研究：
Topoisomerase I/II inhibitor 4 (compound F16) (10-50 mg/kg; i.v.; per 2 days, for 7 days) suppresses tumor growth in the A375 Xenograft Model.Topoisomerase I/II inhibitor 4 (compound F16) of the plasma clearance rate (CL) was 7-fold lower than that of VP-16(0.007 L/min/kg). Topoisomerase I/II inhibitor 4 has a delayed elimination half-life of 151 min.Animal Model:Female BALB/c nude mice (5?6 weeks)
Dosage:10 and 20 mg/kg
Administration:Intravenous injection; Per 2 days, for 14 days.
Result:Inhibited tumor growth in a melanoma xenograft mouse model and no apparent loss in body weight.
Animal Model:Kunming male mice
Dosage:10 mg/kg
Administration:Intravenous injection; for 5 , 15 , 30 , 60 , 120 , 240 and 360 min.
Result:1.19ParameterF16VP-16
Dose (i.v.) mg/kg1010
Cmax (ng/mL)2695217712
Tmax (min)55
AUCplasma (min*ng/mL)2878363409528
T1/2 (min)15145
Vd (L/Kg)0.23410.432
CL (L/min/kg)0.0010.007
体外研究：
Topoisomerase I/II inhibitor 4 (compound F16) (0-100 μM) could intercalate into DNA to inhibit enzymatic activity and inhibit Topo I and II activities in a dose-dependent manner.Topoisomerase I/II inhibitor 4 (compound F16) shows a high-expression level of Topo I and II enzymes in A375 and HCT116 cells and exhibits potent anti-proliferative activity with IC50 values of 20 and 50 nM, respectively, 10-fold lower than L02.Topoisomerase I/II inhibitor 4 (compound F16) (0-40 nM, A375 cell) inhibits cancer cell colony formation, invasion, migration and induces cell apoptosis.
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