Irinotecan

Catalog No.S1198

Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

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Irinotecan Chemical Structure

Irinotecan Chemical Structure
Molecular Weight: 586.68

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Product Information

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Product Description

Biological Activity

Description Irinotecan is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
Targets Topo I [1]
(LoVo, HT-29 cells)
In vitro 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. [1] 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. [2] Irinotecan is also converted to SN-38 in intestines, plasma and tumor tissues. [3] Irinotecan is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38. [4]
In vivo In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. [5] 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. [6]
Features Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.

Protocol(Only for Reference)

Cell Assay:

[1]

Cell lines LoVo and HT-29 cells
Concentrations 0 μM -100 μM
Incubation Time 48 hours
Method

Exponentially growing cells (LoVo and HT-29 cells) are seeded in 20 cm2 Petri dishes with an optimal cell number for each cell line (2 × 104 for LoVo cells, 105 for HT-29 cells). They are treated 2 days later with increasing concentrations of Irinotecan or SN-38 for one cell doubling time (24 hours for LoVo cells, 40 hours for HT-29 cells). After washing with 0.15 M NaCl, the cells are further grown for two doubling times in normal medium, detached from the support with trypsin-EDTA and counted in a hemocytometer. The IC50 values are then estimated as the Irinotecan or SN-38 concentrations responsible for 50% growth inhibition as compared with cells incubated without Irinotecan or SN-38.

Animal Study:

[5]

Animal Models Female nude mice with COLO 320 and WiDr xenografts
Formulation 0.9% NaCl
Dosages 20 mg/kg
Administration Administered via i.p.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDogMonkeyBaboon
Weight (kg)0.020.151.80.40.0810312
Body Surface Area (m2)0.0070.0250.150.050.020.50.240.6
Km factor361285201220
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.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Pavillard V, et al. Cancer Chemother Pharmacol. 2002, 49(4), 329-335.

[2] Tobin P, et al. Br J Clin Pharmacol. 2006, 62(1), 122-129.

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Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2015-06-27)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02192359 Not yet recruiting Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult  ...more Adult Anaplastic Astrocytoma|Adult Anaplastic Oligodendroglioma|Adult Giant Cell Glioblastoma|Adult Glioblastoma|Adult Gliosarcoma|Recurrent Adult Brain Tumor City of Hope Medical Center|National Cancer Institute (NCI) July 2015 Phase 1
NCT02450656 Recruiting Colorectal Neoplasms|Gastrointestinal Neoplasms|Pancreatic Neoplasms|Carcinoma, Non-Small-Cell Lung The Netherlands Cancer Institute|AstraZeneca|Boehringer I  ...more The Netherlands Cancer Institute|AstraZeneca|Boehringer Ingelheim June 2015 Phase 1|Phase 2
NCT02110953 Not yet recruiting Liver Metastases|Mucinous Adenocarcinoma of the Colon|Mucinous Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Signet R  ...more Liver Metastases|Mucinous Adenocarcinoma of the Colon|Mucinous Adenocarcinoma of the Rectum|Recurrent Colon Cancer|Recurrent Rectal Cancer|Signet Ring Adenocarcinoma of the Colon|Signet Ring Adenocarcinoma of the Rectum|Stage IVA Colon Cancer|Stage IVA Rectal Cancer|Stage IVB Colon Cancer|Stage IVB Rectal Cancer Fox Chase Cancer Center|National Cancer Institute (NCI) June 2015 Phase 1
NCT02345460 Not yet recruiting Pancreatic Adenocarcinoma|Poorly Differentiated Malignant Neoplasm|Resectable Pancreatic Cancer|Stage IA Pancreatic Cancer|Stage IB Pancreatic Canc  ...more Pancreatic Adenocarcinoma|Poorly Differentiated Malignant Neoplasm|Resectable Pancreatic Cancer|Stage IA Pancreatic Cancer|Stage IB Pancreatic Cancer|Stage IIA Pancreatic Cancer|Stage IIB Pancreatic Cancer|Stage III Pancreatic Cancer|Undifferentiated Pancreatic Carcinoma Case Comprehensive Cancer Center|National Cancer Institut  ...more Case Comprehensive Cancer Center|National Cancer Institute (NCI) May 2015 Phase 2
NCT02366819 Recruiting Esophageal Adenocarcinoma|Gastric Adenocarcinoma|Stage IIB Gastric Cancer|Stage IIIA Esophageal Adenocarcinoma|Stage IIIA Gastric Cancer|Stage IIIB  ...more Esophageal Adenocarcinoma|Gastric Adenocarcinoma|Stage IIB Gastric Cancer|Stage IIIA Esophageal Adenocarcinoma|Stage IIIA Gastric Cancer|Stage IIIB Esophageal Adenocarcinoma|Stage IIIB Gastric Cancer|Stage IIIC Esophageal Adenocarcinoma|Stage IIIC Gastric Cancer University of Chicago|National Cancer Institute (NCI) April 2015 Phase 4

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Chemical Information

Download Irinotecan SDF
Molecular Weight (MW) 586.68
Formula

C33H38N4O6

CAS No. 97682-44-5
Storage 3 years -20℃powder
6 months-80℃in solvent
Synonyms CPT-11
Solubility (25°C) * In vitro DMSO 7 mg/mL (11.93 mM)
Water <1 mg/mL (<1 mM)
Ethanol <1 mg/mL (<1 mM)
In vivo 30% propylene glycol, 5% Tween 80, 65% D5W 30 mg/mL
* <1 mg/ml means slightly soluble or insoluble.
* 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.
Chemical Name (4S)​-​4,​11-​diethyl-​3,​4,​12,​14-​tetrahydro-​4-​hydroxy-​3,​14-​dioxo-​1H-​pyrano[3',​4':6,​7]​indolizino[1,​2-​b]​quinolin-​9-​yl-[1,​4'-​bipiperidine]​-​1'-​carboxylic acid

Customer Product Validation (1)


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Rating
Source Dr. Mikhail Menshikov of Cardiology Research Center. Irinotecan purchased from Selleck
Method Cell viability assay
Cell Lines pancreatic cancer cells
Concentrations 0-100 μM
Incubation Time 72 h
Results Irinotecan potently inhibited the survival of Panc1 cells in a dose-dependent manner.

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