Irinotecan (CPT-11)

Catalog No.S1198 Synonyms: (+)-Irinotecan,CPT-11

For research use only.

Irinotecan (CPT-11, (+)-Irinotecan) is a topoisomerase I inhibitor for LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.

Irinotecan (CPT-11) Chemical Structure

CAS No. 97682-44-5

Selleck's Irinotecan (CPT-11) has been cited by 25 publications

Purity & Quality Control

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Biological Activity

Description Irinotecan (CPT-11, (+)-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 NXT4OW1O[3m2b4TvfIlkcXS7IHHzd4F6 NInkSGcyOCEQvF2= MlfpSG1UVw>? NESzU2JKTDVyPUW0NEBvVQ>? NGXuWHYyOTl4NUO2Ni=>
VM46 NV;nOlhC[3m2b4TvfIlkcXS7IHHzd4F6 MWixNEDPxE1? NFX1fm9FVVOR MnH1TWQ2OD1{MkCgcm0> M3;I[VEyQTZ3M{[y
MCF-7ADR NXHhTYJT[3m2b4TvfIlkcXS7IHHzd4F6 M3jOflExKM7:TR?= MmnBSG1UVw>? MV3JSFUxRjVyMDDuUS=> Ml\ZNVE6PjV|NkK=
L1210 MV\jfZRwfG:6aXPpeJkh[XO|YYm= MojRTWM2OD1zLkKgxtVO M33PS|E5PDZ7MkO=
RPMI8402 M{SyPIN6fG:2b4jpZ4l1gSCjc4PhfS=> NHPtb5IyODBizszN NECyZmFKSzVyPUW3NEBvVQ>? NVLsZoRvOTJ5NEe3PVg>
A-549 NX;1bYd3[3m2b4TvfIlkcXS7IHHzd4F6 MmDrglIxKM7:TR?= MUTEUXNQ NFOxU3JKSzVyPU[uOVI5KM7:TR?= NIXPXGUyQDJyN{e0PC=>
LOVO MVvjfZRwfG:6aXPpeJkh[XO|YYm= MUf+NlAh|ryP M4D3dmROW09? MmW4TWM2OD17LkCxOUDPxE1? MU[xPFIxPzd2OB?=
MCF7 MV7jfZRwfG:6aXPpeJkh[XO|YYm= MVv+NlAh|ryP NInCdmZFVVOR NGPS[VdKSzVyPUG3MlQxOyEQvF2= M4Pib|E5OjB5N{S4
LS174T M3e4Nmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NHviTGRFVVOR MVHJR|UxRTFwMU[g{txO M4XKOVE5PDd7MUG4
KB3-1 MVTjfZRwfG:6aXPpeJkh[XO|YYm= MUnJR|UxRTBwNkig{txO M2rS[VE5PzdzOUOw
KBV-1 MVXjfZRwfG:6aXPpeJkh[XO|YYm= MUDJR|UxRTRyIN88US=> MUmxPFc4OTl|MB?=
KBH5.0 NFPwdZVkgXSxdH;4bYNqfHliYYPzZZk> Mm\ETWM2OD15LkSg{txO M2H5TVE5PzdzOUOw
Hep G2 NILIZ|NIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MnPlglExKM7:TR?= M3nQU2ROW09? MXfJR|UxRTVwOUSg{txO M3\ONlE6Pzl4OUW2
Hep 3B NUKxd3RDT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NGn5WWV,OTBizszN MUjEUXNQ NXju[WExUUN3ME20Mlc{KM7:TR?= NXfWWnRkOTl5OU[5OVY>
Hep 2.2. MWfHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? MYX+NVAh|ryP MnXFSG1UVw>? MkPiTWM2OD5zMDFOwG0> MUSxPVc6Pjl3Nh?=
A549 MXTjfZRwfG:6aXPpeJkh[XO|YYm= M1XrfGROW09? MmTJTWM2OD12Lk[xJO69VQ>? MXWyNFM4OTF6Mx?=
MDA-MB-435 NHn2RZBkgXSxdH;4bYNqfHliYYPzZZk> MljKSG1UVw>? M4jRdWlEPTB;MT6xOEDPxE1? NFjXbHUzODN5MUG4Ny=>
LOVO M1HXXoN6fG:2b4jpZ4l1gSCjc4PhfS=> NXTNO3N[TE2VTx?= MVrJR|UxRTRwOUmg{txO MUCyNFM4OTF6Mx?=
MDA-MB-435 MmfUZ5l1d3SxeHnjbZR6KGG|c3H5 MVzEUXNQ M4n4WGlEPTB;MUeg{txO MmD1NlA6PDJ2OUC=
NCI60 NX3VO4F{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= NV22[2VPTE2VTx?= MVrHTVUxRTF2LkGyOVQh|ryP NUXwOmhGOjFyM{WzN|Q>
H460 MVzjfZRwfG:6aXPpeJkh[XO|YYm= NWm3NI5uTE2VTx?= MYnJR|UxRTBwMEG1JO69VQ>? NFfvU4wzOTN2MU[3OC=>
PC-3 NU\lSmVL[3m2b4TvfIlkcXS7IHHzd4F6 MXPEUXNQ MV3JR|UxRTBwMkKg{txO MlTJNlE{PDF4N{S=
HT29 NGDxfJpkgXSxdH;4bYNqfHliYYPzZZk> NHLqR|hFVVOR NWO2c4Z5UUN3ME2wMlAxPCEQvF2= NYLIUHhZOjF|NEG2O|Q>
SK-MEL-2 MkTUZ5l1d3SxeHnjbZR6KGG|c3H5 NInQ[mFFVVOR MUfJR|UxRTBwMTFOwG0> NXXENZRFOjF|NEG2O|Q>
A375 MX;jfZRwfG:6aXPpeJkh[XO|YYm= MVzEUXNQ NUfKSI9HUUN3ME2wMlAxPCEQvF2= NYmySld[OjF|NEG2O|Q>
Malme-3M M3PjOIN6fG:2b4jpZ4l1gSCjc4PhfS=> NEXkZWRFVVOR NYDaPY9NUUN3ME2wMlIh|ryP NFzNflQzOTN2MU[3OC=>
DU 145 MYjjfZRwfG:6aXPpeJkh[XO|YYm= NEDsdGlFVVOR Mn3rTWM2OD1yLkKg{txO M2KzbVIyOzRzNke0
LNCaP MXnjfZRwfG:6aXPpeJkh[XO|YYm= NXXYTZh3TE2VTx?= NWnQe5E2UUN3ME2wMlAxQSEQvF2= NIDCPJozOTN2MU[3OC=>
IGROV-1 NYqxTIc5[3m2b4TvfIlkcXS7IHHzd4F6 MYTEUXNQ NHnMbY9KSzVyPUCuNFMh|ryP M3jrU|IyOzRzNke0
KB NYLWTHVM[3m2b4TvfIlkcXS7IHHzd4F6 M{\TWp4zOCEQvF2= M3m0d2ROW09? NETOSHlKSzVyPUmuPFMh|ryP NVvOTnhFOjJyN{myOVQ>
KB-vin NWD5dHNG[3m2b4TvfIlkcXS7IHHzd4F6 NHrzO4Z,OjBizszN MlvHSG1UVw>? NHvoOG5KSzVyPkKwJO69VQ>? NHO2OlQzOjB5OUK1OC=>
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 (from reference)

Cell Research:

[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 Research:

[5]

  • Animal Models: Female nude mice with COLO 320 and WiDr xenografts
  • Dosages: 20 mg/kg
  • Administration: Administered via i.p.

Solubility (25°C)

In vitro

Chemical Information

Molecular Weight 586.68
Formula

C33H38N4O6

CAS No. 97682-44-5
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CCC1=C2CN3C(=CC4=C(C3=O)COC(=O)C4(CC)O)C2=NC5=C1C=C(C=C5)OC(=O)N6CCC(CC6)N7CCCCC7

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05277766 Not yet recruiting Drug: PIPAC with Nal-IRI Peritoneal Carcinomatosis|Peritoneal Metastases|Colorectal Cancer|Small Bowel Cancer|Appendix Cancer|Gastric Cancer|Pancreatic Cancer|Bile Duct Cancer University Hospital Ghent|Kom Op Tegen Kanker|University Ghent September 2022 Phase 1
NCT05379790 Recruiting Drug: Irinotecan|Drug: CAPOX Gastric Cancer|Peritoneal Metastases Erasmus Medical Center May 25 2022 Phase 1
NCT05101096 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced Solid Tumors or Triple-negative Breast Cancer Gilead Sciences October 20 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-08-01)

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