Irinotecan HCl Trihydrate
Catalog No.S2217 Synonyms: CPT-11 HCl Trihydrate
Molecular Weight(MW): 677.18
Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.
Cited by 30 Publications
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Choose Selective Topoisomerase Inhibitors
|Description||Irinotecan prevents DNA from unwinding by inhibition of topoisomerase 1.|
|Features||Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.|
Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. Irinotecan induces similar amounts of cleavable complexes at its IC50 in LoVo cells and HT-29 cell lines. SN-38 induces a concentration-dependent formation of cleavable complexes, which is not significantly different in LoVo cells and HT-29 cell lines. Cell accumulation of Irinotecan is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells.  The lactone E-ring of Irinotecan and SN-38 hydrolyses reversibly in aqueous solutions, and the interconversion between the lactone and carboxylate forms is dependent on pH and temperature. Liver is primarily responsible for the activation of Irinotecan to SN-38. At equal concentrations of Irinotecan and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from Irinotecan in both tumour and normal tissue.  Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues.  Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. 
|In vivo||In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%.  A single dose of Irinotecan significantly increases amounts of topoisomerase I covalently bound to DNA in stomach, duodenum, colon and liver. Concomitantly, the Irinotecan-treated group shows significantly higher amounts of DNA strand breaks in colon mucosa cells compared to the control group. |
-  Pavillard V, et al. Cancer Chemother Pharmacol. 2002, 49(4), 329-335.
-  Tobin P, et al. Br J Clin Pharmacol. 2006, 62(1), 122-129.
-  Shingyoji M, et al. Cancer Sci. 2004, 95(6), 537-540.
|In vitro||DMSO||100 mg/mL (147.67 mM)|
|Ethanol||7 mg/mL (10.33 mM)|
|Water||1 mg/mL (1.47 mM)|
|In vivo||Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
For best results, use promptly after mixing.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
|Synonyms||CPT-11 HCl Trihydrate|
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Clinical Trial Information
|NCT Number||Recruitment||interventions||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT04074343||Recruiting||Drug: TAS-102|Drug: Irinotecan||Gastric Adenocarcinoma|GastroEsophageal Cancer||University of California Irvine|Taiho Pharmaceutical Co. Ltd.||August 28 2019||Phase 1|
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