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.

Size Price Stock Quantity  
In DMSO USD 90 In stock
USD 70 In stock
USD 120 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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Notes:

2. For more details, such as half maximal inhibitory concentrations (IC50s) and working concentrations of each inhibitor, please click on the link of the inhibitor of interest.
3. "+" indicates inhibitory effect. Increased inhibition is marked by a higher "+" designation.
4. Orange "√" refers to compounds which do inhibitory effects on the related isoform, but without specific value.

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 MUjjfZRwfG:6aXPpeJkh[XO|YYm= MWWxNEDPxE1? MWLEUXNQ M1TveGlFPTB;NUSwJI5O NH;yOZIyOTl4NUO2Ni=>
VM46 M1zoSYN6fG:2b4jpZ4l1gSCjc4PhfS=> NVrxZopKOTBizszN NFT0eIZFVVOR NHzUZpRKTDVyPUKyNEBvVQ>? MXixNVk3PTN4Mh?=
MCF-7ADR NX;Y[ohT[3m2b4TvfIlkcXS7IHHzd4F6 M3zmZ|ExKM7:TR?= M3q1fWROW09? MofpTWQ2OD53MECgcm0> NIrCVJAyOTl4NUO2Ni=>
L1210 M{TuVoN6fG:2b4jpZ4l1gSCjc4PhfS=> MnnvTWM2OD1zLkKgxtVO Mlq5NVg1Pjl{Mx?=
RPMI8402 NXjoVYZV[3m2b4TvfIlkcXS7IHHzd4F6 NGDuRXYyODBizszN MoWxTWM2OD13N{Cgcm0> NHjGNZEyOjd2N{e5PC=>
A-549 MknmZ5l1d3SxeHnjbZR6KGG|c3H5 M1vkT54zOCEQvF2= MUHEUXNQ NFn6WmFKSzVyPU[uOVI5KM7:TR?= M{DBfFE5OjB5N{S4
LOVO MYLjfZRwfG:6aXPpeJkh[XO|YYm= MV3+NlAh|ryP MXfEUXNQ NGT4NFFKSzVyPUmuNFE2KM7:TR?= MnfKNVgzODd5NEi=
MCF7 NUO4dotu[3m2b4TvfIlkcXS7IHHzd4F6 MlX4glIxKM7:TR?= MV7EUXNQ M17RbGlEPTB;MUeuOFA{KM7:TR?= NXi4WZNbOTh{MEe3OFg>
LS174T NUP1eZJoT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= Mn\SSG1UVw>? MkHYTWM2OD1zLkG2JO69VQ>? NV\xUnAxOTh2N{mxNVg>
KB3-1 MmXsZ5l1d3SxeHnjbZR6KGG|c3H5 NWriSJBYUUN3ME2wMlY5KM7:TR?= NV\0UXFwOTh5N{G5N|A>
KBV-1 NIK4WHZkgXSxdH;4bYNqfHliYYPzZZk> NWCwS5pYUUN3ME20NEDPxE1? M2PqTlE5PzdzOUOw
KBH5.0 M{jBToN6fG:2b4jpZ4l1gSCjc4PhfS=> NVzySHVnUUN3ME23MlQh|ryP M3Ho[FE5PzdzOUOw
Hep G2 NYHBTpN[T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXf+NVAh|ryP NFy0NoNFVVOR MorrTWM2OD13Lkm0JO69VQ>? NITWSIMyQTd7Nkm1Oi=>
Hep 3B MnHlS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MUX+NVAh|ryP MnvlSG1UVw>? NYW3dmdWUUN3ME20Mlc{KM7:TR?= NY[weZNFOTl5OU[5OVY>
Hep 2.2. MUXHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MkDpglExKM7:TR?= MkDFSG1UVw>? NVHUVYNLUUN3ME6xNEDPxE1? M2rudlE6Pzl4OUW2
A549 NGPYT5lkgXSxdH;4bYNqfHliYYPzZZk> NGnaXXdFVVOR NFz1NmFKSzVyPUSuOlEh|ryP NGfDZowzODN5MUG4Ny=>
MDA-MB-435 NULOfmJX[3m2b4TvfIlkcXS7IHHzd4F6 NVnFcJVZTE2VTx?= M{PkbGlEPTB;MT6xOEDPxE1? NF;0fm4zODN5MUG4Ny=>
LOVO NGGxdVdkgXSxdH;4bYNqfHliYYPzZZk> MmroSG1UVw>? NXjveIF[UUN3ME20Mlk6KM7:TR?= M{OySFIxOzdzMUiz
MDA-MB-435 M4W1VoN6fG:2b4jpZ4l1gSCjc4PhfS=> MnGySG1UVw>? MWLJR|UxRTF5IN88US=> MYeyNFk1OjR7MB?=
NCI60 NXnwUY0xT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= M3TVUmROW09? MXHHTVUxRTF2LkGyOVQh|ryP NWLVToVIOjFyM{WzN|Q>
H460 M1\LZYN6fG:2b4jpZ4l1gSCjc4PhfS=> MWnEUXNQ M1vw[2lEPTB;MD6wNVUh|ryP NXe4SlJTOjF|NEG2O|Q>
PC-3 MV\jfZRwfG:6aXPpeJkh[XO|YYm= Mn\NSG1UVw>? NVvlSXNlUUN3ME2wMlIzKM7:TR?= MXWyNVM1OTZ5NB?=
HT29 NU\lVFhF[3m2b4TvfIlkcXS7IHHzd4F6 NXzzXms6TE2VTx?= M2PaRmlEPTB;MD6wNFQh|ryP NGPxO5IzOTN2MU[3OC=>
SK-MEL-2 NVL6VFFi[3m2b4TvfIlkcXS7IHHzd4F6 MYjEUXNQ NFzR[GRKSzVyPUCuNUDPxE1? NWHCR|I3OjF|NEG2O|Q>
A375 NIXk[ZlkgXSxdH;4bYNqfHliYYPzZZk> NGHvWnpFVVOR NGP5[GVKSzVyPUCuNFA1KM7:TR?= NH7IW2IzOTN2MU[3OC=>
Malme-3M M{PnTYN6fG:2b4jpZ4l1gSCjc4PhfS=> NGTDXpNFVVOR M2riV2lEPTB;MD6yJO69VQ>? MVGyNVM1OTZ5NB?=
DU 145 NEnlXWtkgXSxdH;4bYNqfHliYYPzZZk> M2XEUWROW09? MVnJR|UxRTBwMjFOwG0> MlrFNlE{PDF4N{S=
LNCaP NGTMOZlkgXSxdH;4bYNqfHliYYPzZZk> M4LPfGROW09? NIP2eGZKSzVyPUCuNFA6KM7:TR?= NF\zelQzOTN2MU[3OC=>
IGROV-1 NEjpZ5lkgXSxdH;4bYNqfHliYYPzZZk> MmexSG1UVw>? NHf3U5lKSzVyPUCuNFMh|ryP MlzBNlE{PDF4N{S=
KB NV2wbXh7[3m2b4TvfIlkcXS7IHHzd4F6 M3TqUp4zOCEQvF2= M1vuUGROW09? NUG5N3VKUUN3ME25Mlg{KM7:TR?= NYf0fGV[OjJyN{myOVQ>
KB-vin NVe5Oo0y[3m2b4TvfIlkcXS7IHHzd4F6 M3T2cJ4zOCEQvF2= M2XaXWROW09? NHv1PHhKSzVyPkKwJO69VQ>? NFnRWVAzOjB5OUK1OC=>

... 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
+ 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
+ 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
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 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
NCT02747537 Not yet recruiting Pediatric Solid Tumors Washington University School of Medicine July 2016 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID