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.

Price Stock Quantity  
USD 90 In stock
USD 70 In stock
USD 120 In stock
Bulk Inquiry

Massive Discount Available

Free Overnight Delivery on all orders over $ 500.

Irinotecan Chemical Structure

Irinotecan Chemical Structure
Molecular Weight: 586.68

Validation & Quality Control

2 customer reviews :

Quality Control & MSDS

Related Compound Libraries

Product Information

  • Compare Topoisomerase Inhibitors
    Compare Topoisomerase Products
  • Research Area

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]
Cell Data
Cell LinesAssay TypeConcentrationIncubation TimeFormulationActivity DescriptionPMID
Hep 3BNFnFNYlIem:5dHigbY5pcWKrdH;yfUBie3OjeR?=NUf6N4lqhjFyIN88US=>M1vmeWROW09?MX3JR|UxRTRwN{Og{txONX\OVFFWOTl5OU[5OVY>
Hep 2.2.MVvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>?NXfwbJhMhjFyIN88US=>M3X6R2ROW09?NXHRTJo1UUN3ME6xNEDPxE1?MYixPVc6Pjl3Nh?=
DU 145NVj6dW44[3m2b4TvfIlkcXS7IHHzd4F6M3\5e2ROW09?NITQR|JKSzVyPUCuNkDPxE1?NUj6TpNnOjF|NEG2O|Q>

... Click to View More Cell Line Experimental Data

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:


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

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:


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 pigHamsterDog
Weight (kg)
Body Surface Area (m2)0.0070.0250.
Km factor36128520
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] 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.

view more

Clinical Trial Information( data from, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
Start Date Phases
NCT02782182 Not yet recruiting Pancreatic Ductal Adenocarcinoma (PDAC) University of Chicago September 2016 --
NCT02677116 Not yet recruiting Neoplasm Metastasis Eli Lilly and Company August 2016 Phase 1
NCT02611024 Not yet recruiting Advanced Solid Tumors PharmaMar August 2016 Phase 1
NCT02842580 Active, not recruiting Colorectal Neoplasms Federation Francophone de Cancerologie Digestive July 2016 Phase 2
NCT02848794 Not yet recruiting High-grade Glioma The First Peoples Hospital of Lianyungang|Shandong Cancer  ...more The First Peoples Hospital of Lianyungang|Shandong Cancer Hospital and Institute|The Affiliated Hospital of Medical College of Qingdao University|Yankuang Group General Hospital|Lianyungang Hospital Affiliated Bengbu Medical College|Suzhou Kowloon Hospital July 2016 Phase 1|Phase 2

view more

Chemical Information

Download Irinotecan SDF
Molecular Weight (MW) 586.68


CAS No. 97682-44-5
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms CPT-11
Solubility (25°C) * In vitro DMSO 7 mg/mL (11.93 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
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

Tech Support

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.

Tel: +1-832-582-8158 Ext:3

If you have any other enquiries, please leave a message.

* Indicates a Required Field

Related Topoisomerase Products

  • SCR7

    SCR7 is a specific DNA Ligase IV inhibitor, which blocks nonhomologous end-joining (NHEJ).

  • Blasticidin S HCl

    Blasticidin S HCl is a nucleoside antibiotic isolated from Stretomyces girseochromogenes, and acts as a DNA and protein synthesis inhibitor, used to select transfected cells carrying bsr or BSD resistance genes.

  • LMK-235

    LMK-235 is a selective inhibitor of HDAC4 and HDAC5 with IC50 of 11.9 nM and 4.2 nM, respectively.

  • Doxorubicin (Adriamycin)

    Doxorubicin (Adriamycin) is an antibiotic agent that inhibits DNA topoisomerase II and induces DNA damage and apoptosis in tumor cells.

  • Etoposide

    Etoposide is a semisynthetic derivative of podophyllotoxin, which inhibits DNA synthesis via topoisomerase II inhibition activity.

  • Camptothecin

    Camptothecin is a specific inhibitor of DNA topoisomerase I (Topo I) with IC50 of 0.68 μM in a cell-free assay. Phase 2.

  • Daunorubicin HCl

    Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM in a cell-free assay.

  • SN-38

    SN-38 is an active metabolite of CPT-11, inhibits DNA topoisomerase I, DNA synthesis and causes frequent DNA single-strand breaks.

  • Topotecan HCl

    Topotecan HCl is a topoisomerase I inhibitor for MCF-7 Luc cells and DU-145 Luc cells with IC50 of 13 nM and 2 nM in cell-free assays, respectively.

    Features:Topotecan is a water-soluble derivative of camptothecin.

  • Idarubicin HCl

    Idarubicin HCl is a hydrochloride salt form of Idarubicin which is an anthracycline antibiotic and a DNA topoisomerase II (topo II) inhibitor for MCF-7 cells with IC50 of 3.3 ng/mL in a cell-free assay.

    Features:Idarubicin is a substrate for CYP450 2D6 and 2C9.

Recently Viewed Items

Tags: buy Irinotecan | Irinotecan ic50 | Irinotecan price | Irinotecan cost | Irinotecan solubility dmso | Irinotecan purchase | Irinotecan manufacturer | Irinotecan research buy | Irinotecan order | Irinotecan mouse | Irinotecan chemical structure | Irinotecan mw | Irinotecan molecular weight | Irinotecan datasheet | Irinotecan supplier | Irinotecan in vitro | Irinotecan cell line | Irinotecan concentration | Irinotecan nmr
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
Contact Us