Inhibition of recombinant human full-length N-terminal His-tagged Tdp1 expressed in Escherichia coli BL21 (DE3) using 5'-(5,6 FAM-aac gtc agg gtc ttc c-BHQ1)-3' as substrate measured every 1 min for 7 mins by fluorimetric method
Inhibition of Tdp1 in human MCF7 cells assessed as potentiation of topotecan-induced antiproliferative activity by measuring increase in maximal inhibition above aditivity at 1 uM after 3 days by [3H]-thymidine incorporation assay
Inhibition of Tdp1 in mouse LLTC cells assessed as potentiation of topotecan-induced antiproliferative activity by measuring increase in maximal inhibition above aditivity at 1 uM after 3 days by [3H]-thymidine incorporation assay
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as state and behavioral changes at 100 mg/kg, ig administered as single dose in presence of topotecan
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as change in body weight at 100 mg/kg, ig administered as single dose (Rvb = 90%)
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as change in body weight at 100 mg/kg, ig administered as single dose in presence of topotecan (Rvb = 90%)
Cytotoxicity against C57BL mouse LLC cells implanted in C57BL/6 mouse assessed as tumor weight at 100 mg/kg, ig administered as single dose measured 17 days post transplantation (Rvb = 3.3 +/- 0.28 g)
Potentiation of topotecan-induced anticancer activity against C57BL mouse LLC cells implanted in C57BL/6 mouse assessed as tumor weight at 100 mg/kg, ig administered as single dose measured 17 days post transplantation (Rvb = 2.9 +/- 0.28 g)
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as liver index at 100 mg/kg, ig administered as single dose measured 17 days post-transplantation in presence of topotecan (Rvb = 5.8 +/- 0.38%)
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as liver index at 100 mg/kg, ig administered as single dose measured 17 days post-transplantation (Rvb = 5.8 +/- 0.38%)
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as spleen weight at 100 mg/kg, ig administered as single dose measured 17 days post-transplantation in presence of topotecan (Rvb = 252 +/- 12 mg)
Toxicity in C57BL/6 mouse implanted with C57BL mouse LLC cells assessed as spleen weight at 100 mg/kg, ig administered as single dose measured 17 days post-transplantation (Rvb = 252 +/- 12 mg)
Cytotoxicity against C57BL mouse LLC cells implanted in C57BL/6 mouse assessed as effect on number of metastatic nodules in lung at 100 mg/kg, ig administered as single dose measured 17 days post transplantation by microscopic analysis