- 貨號 Cat. No.
- S1198
- 規格 Size
- 10mM/1mLã€100mgã€200mg
- 品牌 Brand
- Selleckchem
Description
Irinotecan
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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10mM/1mLIn DMSO |
USD 113 |
In stock |
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100mg |
USD 88 |
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200mg |
USD 151 |
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Distributor Tel: +886-2-2827-1197jimmy@new.abscience.com.tw
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. |
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Targets |
LoVo cells |
HT-29 cells |
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IC50 |
15.8 μM |
5.17 μM [1] |
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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] |
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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] |
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Features |
Irinotecan is a prodrug that is used to treat metastatic colorectal cancer. |
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Protocol(Only for Reference)
Cell Assay: [1]
Cell lines |
LoVo and HT-29 cells |
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Concentrations |
0 μM -100 μM |
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Incubation Time |
48 hours |
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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. |
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Animal Study: [5]
Animal Models |
Female nude mice with COLO 320 and WiDr xenografts |
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Dosages |
20 mg/kg |
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Administration |
Administered via i.p. |
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Solubility |
30% propylene glycol, 5% Tween 80, 65% D5W, 30 mg/mL |
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1
References
Clinical Trial Information( data from http://clinicaltrials.gov)
NCT Number |
Recruitment |
Conditions |
Sponsor
/Collaborators |
Start Date |
Phases |
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NCT01996306 |
Not yet recruiting |
Colorectal Neoplasms|Neoplasm Metastasis|Intestinal Neoplasms|Gastrointestinal Neoplasms|Digestive System Neoplasms |
Epidemiological and Clinical Research Information Network |
2013-12 |
Phase 3 |
NCT02015754 |
Not yet recruiting |
Colorectal Cancer |
Sidney Kimmel Comprehensive Cancer Center |
2013-12 |
Phase 2 |
NCT01928290 |
Not yet recruiting |
Stomach Neoplasms|Esophageal Neoplasms |
Washington University School of Medicine |
2013-12 |
Phase 2 |
NCT01959139 |
Not yet recruiting |
Metastatic Pancreatic Adenocarcinoma |
Southwest Oncology Group|National Cancer Institute (NCI)|Halozyme Therapeutics |
2013-12 |
Phase 1|Phase 2 |
NCT01992705 |
Not yet recruiting |
Resectable Pancreatic Cancer |
University of Maryland |
2014-01 |
Phase 0 |
Download Irinotecan SDF
Molecular Weight (MW) |
586.68 |
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Formula |
C33H38N4O6
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CAS No. |
97682-44-5 |
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Storage |
3 years -20℃Powder |
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6 months-80℃in DMSO |
Syonnyms |
Camptosar, Campto |
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Solubility (25°C) * |
In vitro |
DMSO |
7 mg/mL (11 mM) |
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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. |
Stock Solution (1ml DMSO) |
1mM |
10mM |
20mM |
30mM |
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Mass(mg) |
0.58668 |
5.8668 |
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Customer Reviews (1)
Click to enlarge |
Rating |
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Source |
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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