Irinotecan hydrochloride trihydrate prevents DNA from unwinding by inhibition of topoisomerase 1. Irinotecan (100 mg/kg) significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver in male Wistar rats. Irinotecan (20 mg/kg i.p.) induces tumor growth inhibition of 92% in COLO 320 xenograft mice model. Irinotecan is activated by hydrolysis to SN-38. The inhibition of topoisomerase I by the active metabolite SN-38 eventually leads to inhibition of both DNA replication and transcription. Irinotecan is currently in phase 2 clinical trials for the treatment of Non-small Cell Lung Cancer.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||DMSO 120 mg/mL|
In vivo bioassay to detect irinotecan-stabilized DNA/topoisomerase I complexes in rats.
Barth SW, et al. Biotechnol J. 2010 Mar;5(3):321-7. PMID: 20213647.
Cellular effects of CPT-11 on colon carcinoma cells: dependence on p53 and hMLH1 status.
Magrini R, et al. Int J Cancer. 2002 Sep 1;101(1):23-31. PMID: 12209584.
Interleukin 15 offers selective protection from irinotecan-induced intestinal toxicity in a preclinical animal model.
Cao S, et al. Cancer Res. 1998 Aug 1;58(15):3270-4. PMID: 9699654.
|Related Topoisomerase Products|
Exatecan Mesylate is a water soluble topoisomerase I inhibitor, with an IC50 of 2.2 μM (0.975 μg/mL).
Ellipticine is a DNA intercalating agent and a DNA topoisomerase II inhibitor.
Pixantrone dimaleate is a topoisomerase II inhibitor and DNA intercalator, with anti-tumor activity.
10-Hydroxycamptothecin is a cell-permeable powerful DNA topoisomerase I inhibitor. It has selective inhibitory effect on the phosphorylation of histone H1 and H3, but less effect on other histones.
7-Ethyl Camptothecin is an anti-cancer chemical that exhibits a strong activity against various murine tumors through Topo I (topoisomerase) inhibition.
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