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.
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Growth inhibitory effects of Irinotecan in human pancreatic cancer cells. Panc1 cells were plated in triplicates into 48-well plates at a density of 10,000 cells/ml. After 24 hours, complete culture medium was changed into fresh low-serum-containing medium (1% FBS) containing DMSO (control) or indicated doses of Irinotecan (Selleckchem). Cell viability 72 hours after treatment was determined by AlamarBlue assay (Invitrogen) according to manufacturer's instructions. Results are expressed as percentages of control, which was arbitrarily assigned 100% viability, and represented as the mean ± standard deviation (SD) of the tripicate wells.
Dr. Mikhail Menshikov of Cardiology Research Center. Irinotecan HCl Trihydrate purchased from Selleck.
Purity & Quality Control
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 individually and in order:
* 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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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).
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* When preparing stock solutions always use the batch-specific molecular weight of the product found on the vial label and MSDS / COA (available online).
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01928290||Recruiting||Stomach Neoplasms|Esophageal Neoplasms||Washington University School of Medicine||November 8, 2013||Phase 2|
|NCT01336985||Terminated||Neoplasm Metastases|Melanoma|Colorectal Neoplasms||National Institutes of Health Clinical Center (CC)||March 28, 2011||Phase 1|
|NCT02316496||Terminated||Colorectal Cancer Metastatic||Groupe Cooperateur Multidisciplinaire en Oncologie (GERCOR)||September 23, 2015||Phase 2|
|NCT02975882||Not yet recruiting||Childhood Solid Neoplasm|Recurrent Central Nervous System Neoplasm|Recurrent Solid Neoplasm|Refractory Central Nervous System Neoplasm||Childrens Oncology Group|National Cancer Institute (NCI)||September 2017||Phase 1|
|NCT02967289||Not yet recruiting||Colon Cancer (High-risk Stage III; pT4N1 or pT1 to 4 N2)||UNICANCER|Canadian Cancer Trials Group||January 2017||Phase 3|
|NCT03009058||Not yet recruiting||Metastatic Cancer||Immodulon Therapeutics Ltd||January 2017||Phase 1|Phase 2|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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