Irinotecan

Catalog No.S1198 Synonyms: CPT-11

Irinotecan Chemical Structure

Molecular Weight(MW): 586.68

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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In DMSO USD 90 In stock
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2 Customer Reviews

  • Biomaterials, 2015, 72:74-89.. Irinotecan purchased from Selleck.

    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 purchased from Selleck.

Purity & Quality Control

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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.
Features Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
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 Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HCT116 MXLjfZRwfG:6aXPpeJkh[XO|YYm= NHHBR4syOCEQvF2= NEWxUnNFVVOR NVS0XXZCUUR3ME21OFAhdk1? M{LWdlEyQTZ3M{[y
VM46 NYKz[pZs[3m2b4TvfIlkcXS7IHHzd4F6 M2nreVExKM7:TR?= NX;UWGdkTE2VTx?= M4jI[mlFPTB;MkKwJI5O Ml\mNVE6PjV|NkK=
MCF-7ADR MXnjfZRwfG:6aXPpeJkh[XO|YYm= M2LOS|ExKM7:TR?= MWDEUXNQ MYXJSFUxRjVyMDDuUS=> MlLHNVE6PjV|NkK=
L1210 MUXjfZRwfG:6aXPpeJkh[XO|YYm= NGjFW3hKSzVyPUGuNkDDvU1? MUixPFQ3QTJ|
RPMI8402 NWHMcZBn[3m2b4TvfIlkcXS7IHHzd4F6 MV6xNFAh|ryP MYXJR|UxRTV5MDDuUS=> MnfBNVI4PDd5OUi=
A-549 NHjPOnlkgXSxdH;4bYNqfHliYYPzZZk> MVX+NlAh|ryP MoLySG1UVw>? M3\rXWlEPTB;Nj61Nlgh|ryP NUXyepJwOTh{MEe3OFg>
LOVO NGnnZXBkgXSxdH;4bYNqfHliYYPzZZk> NYjofVhvhjJyIN88US=> MVTEUXNQ M2ez[mlEPTB;OT6wNVUh|ryP MVSxPFIxPzd2OB?=
MCF7 MXvjfZRwfG:6aXPpeJkh[XO|YYm= MWX+NlAh|ryP MnXNSG1UVw>? MWjJR|UxRTF5LkSwN{DPxE1? MV:xPFIxPzd2OB?=
LS174T NGTzTFJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NHraXpBFVVOR Mk\rTWM2OD1zLkG2JO69VQ>? NYXOTI1wOTh2N{mxNVg>
KB3-1 MXHjfZRwfG:6aXPpeJkh[XO|YYm= NFHWbIZKSzVyPUCuOlgh|ryP M{P4R|E5PzdzOUOw
KBV-1 MWfjfZRwfG:6aXPpeJkh[XO|YYm= NYTtSIVoUUN3ME20NEDPxE1? MXixPFc4OTl|MB?=
KBH5.0 M4C4XIN6fG:2b4jpZ4l1gSCjc4PhfS=> MWfJR|UxRTdwNDFOwG0> MXKxPFc4OTl|MB?=
Hep G2 NVyyT5J7T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mo[0glExKM7:TR?= NEnBcpVFVVOR M2P6WWlEPTB;NT65OEDPxE1? NI\ieHoyQTd7Nkm1Oi=>
Hep 3B Ml[xS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NF3KflJ,OTBizszN M3noOWROW09? MoPpTWM2OD12LkezJO69VQ>? NXm4bXM6OTl5OU[5OVY>
Hep 2.2. NXuxUW9jT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NWT0bGZrhjFyIN88US=> MmjOSG1UVw>? NWrQN4FRUUN3ME6xNEDPxE1? MVGxPVc6Pjl3Nh?=
A549 MWrjfZRwfG:6aXPpeJkh[XO|YYm= NIHYRVBFVVOR MlK3TWM2OD12Lk[xJO69VQ>? M4frN|IxOzdzMUiz
MDA-MB-435 MlPRZ5l1d3SxeHnjbZR6KGG|c3H5 NHzL[YJFVVOR MmDaTWM2OD1zLkG0JO69VQ>? MnvpNlA{PzFzOEO=
LOVO M4m5boN6fG:2b4jpZ4l1gSCjc4PhfS=> Ml3YSG1UVw>? NVjaR2duUUN3ME20Mlk6KM7:TR?= NXLYNJlVOjB|N{GxPFM>
MDA-MB-435 MXLjfZRwfG:6aXPpeJkh[XO|YYm= MnTlSG1UVw>? NIOyVWFKSzVyPUG3JO69VQ>? Mn3sNlA6PDJ2OUC=
NCI60 MlmyS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NX7l[WZGTE2VTx?= MnzOS2k2OD1zND6xNlU1KM7:TR?= M4fkfVIyODN3M{O0
H460 M4D4[IN6fG:2b4jpZ4l1gSCjc4PhfS=> NF7HdY5FVVOR NX;ico5uUUN3ME2wMlAyPSEQvF2= MoXXNlE{PDF4N{S=
PC-3 NXfFeHRq[3m2b4TvfIlkcXS7IHHzd4F6 MlvHSG1UVw>? M1rzOGlEPTB;MD6yNkDPxE1? NEWydG8zOTN2MU[3OC=>
HT29 NGTmdFdkgXSxdH;4bYNqfHliYYPzZZk> MnfaSG1UVw>? MYHJR|UxRTBwMEC0JO69VQ>? Mmj1NlE{PDF4N{S=
SK-MEL-2 NGewemVkgXSxdH;4bYNqfHliYYPzZZk> NFH5UZdFVVOR NEn4fWhKSzVyPUCuNUDPxE1? MXqyNVM1OTZ5NB?=
A375 MXvjfZRwfG:6aXPpeJkh[XO|YYm= MlSzSG1UVw>? NXv2W|F{UUN3ME2wMlAxPCEQvF2= NEH5TYczOTN2MU[3OC=>
Malme-3M MXTjfZRwfG:6aXPpeJkh[XO|YYm= M4\pPGROW09? NYj1eFFNUUN3ME2wMlIh|ryP NUTPTplIOjF|NEG2O|Q>
DU 145 MmPsZ5l1d3SxeHnjbZR6KGG|c3H5 M{nzXWROW09? MkDVTWM2OD1yLkKg{txO NV\LWZpGOjF|NEG2O|Q>
LNCaP NVrKUIEx[3m2b4TvfIlkcXS7IHHzd4F6 M4\sWWROW09? MlrhTWM2OD1yLkCwPUDPxE1? MnHZNlE{PDF4N{S=
IGROV-1 NX72O5BG[3m2b4TvfIlkcXS7IHHzd4F6 MnjUSG1UVw>? NXzqbY9WUUN3ME2wMlA{KM7:TR?= MUOyNVM1OTZ5NB?=
KB MX;jfZRwfG:6aXPpeJkh[XO|YYm= NGfZd3R,OjBizszN NFPlb4hFVVOR NV6xV4YzUUN3ME25Mlg{KM7:TR?= NVn6NGllOjJyN{myOVQ>
KB-vin MlzCZ5l1d3SxeHnjbZR6KGG|c3H5 NFnZcFh,OjBizszN MlTmSG1UVw>? M4Dt[WlEPTB-MkCg{txO M13HbFIzODd7MkW0

... 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]

Protocol

Cell Research:

[1]

+ Expand
  • 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.


    (Only for Reference)
Animal Research:

[5]

+ Expand
  • Animal Models: Female nude mice with COLO 320 and WiDr xenografts
  • Formulation: 0.9% NaCl
  • Dosages: 20 mg/kg
  • Administration: Administered via i.p.
    (Only for Reference)

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 Information

Molecular Weight 586.68
Formula

C33H38N4O6

CAS No. 97682-44-5
Storage powder
in solvent
Synonyms CPT-11

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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
NCT03009058 Not yet recruiting Metastatic Cancer Immodulon Therapeutics Ltd January 2017 Phase 1|Phase 2
NCT03017326 Not yet recruiting Hepatoblastoma|Carcinoma, Hepatocellular University of Birmingham|Fundació Institut Germans Trias i Pujol|University of Padua|University of Newcastle Upon-Tyne|University Hospital Munich|University Hospital, Bonn|University of Kiel|University Hospital Tuebingen|Medical University of Gdansk January 2017 Phase 3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID