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Irinotecan Hydrochloride Trihydrate

Cat. No. M2089

Irinotecan Hydrochloride Trihydrate Structure

Synonym: Campto, CPT-11

Size Price Availability Quantity
200mg USD 100 In stock
1g USD 420 In stock
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Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 677.18
Formula C33H38N4O6.HCl.3H2O
CAS Number 136572-09-3
Purity 98.48%
Solubility DMSO 120 mg/mL
Storage at -20°C
References

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.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Irinotecan Hydrochloride Trihydrate, Campto, CPT-11 supplier, Topoisomerase, inhibitors

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