Irinotecan (also known as CPT-11) is a water soluble, semi-synthetic analogue of 20(S)camptothecin (CPT) with promising activity against a range of tumour types. Irinotecan causes cell toxicity by stabilizing a ternary complex between the nuclear enzyme topoisomerase I (topo I) and double-stranded DNA, leading to single and double strand breaks. [Clin Exp Pharmacol Physiol. 1996 Oct-Nov;23(10-11):1000-4.] TopoGEN provides this reagent as a control poison/inhibitor of topoisomerase I. For in vitro cleavage detection, we recommend that the drug be tested over a wide range of uM concentrations; however, cleavages are strongly influenced by the amount of topoisomerase in the reaction as well as the type of assay being employed (SDSK+ vs. Radioactive End Labeled DNA vs. testing for plasmid cleavages). Note that large amounts of enzyme will be required to detect cleavage complex, compared to assays that measure catalytic activity.
Molecular Formula: C33H38N4O6.HCl.3H2O
Molecular Weight: 677.2
TG4101 is supplied already suspended in water at 10 mM (0.25 ml) and is ready for use. The drug is pre-tested and shown to induce topo cleavages using purified human topoisomerase from TopoGEN.
The liquid product is shipped on dry ice. Store at -20°C.
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