Irinotecan (CPT-11)

For research use only.

Catalog No.S1198 Synonyms: (+)-Irinotecan

16 publications

Irinotecan (CPT-11) Chemical Structure

CAS No. 97682-44-5

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.

Selleck's Irinotecan (CPT-11) has been cited by 16 publications

2 Customer Reviews

  • In vitro cell uptake data showing the HA coating on HAC-PFP-DC nanoparticles significantly improves drug delivery into prostasphere and mammosphere cells enriched with CSCs. Fluorescence micrographs of mammosphere cells after incubated with the simple mixture of free DOX&CPT, PFP-DC nanoparticles, and HAC-PFPDC nanoparticles for 3 h at 37℃.

    Biomaterials, 2015, 72:74-89.. Irinotecan (CPT-11) 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 (CPT-11) purchased from Selleck.

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 NX3PVGlP[3m2b4TvfIlkcXS7IHHzd4F6 NGTMRlAyOCEQvF2= MYTEUXNQ M1\wPWlFPTB;NUSwJI5O M4\IOlEyQTZ3M{[y
VM46 Mm\nZ5l1d3SxeHnjbZR6KGG|c3H5 MnTWNVAh|ryP MXrEUXNQ MlrNTWQ2OD1{MkCgcm0> M2W1WVEyQTZ3M{[y
MCF-7ADR NWTuOZNU[3m2b4TvfIlkcXS7IHHzd4F6 MVSxNEDPxE1? MWfEUXNQ MVPJSFUxRjVyMDDuUS=> M3vMcFEyQTZ3M{[y
L1210 MoDwZ5l1d3SxeHnjbZR6KGG|c3H5 M3TtWGlEPTB;MT6yJOK2VQ>? NYW0S3gxOTh2NkmyNy=>
RPMI8402 MlTEZ5l1d3SxeHnjbZR6KGG|c3H5 Ml7CNVAxKM7:TR?= M33IZWlEPTB;NUewJI5O NV30Nm9qOTJ5NEe3PVg>
A-549 M4jTWYN6fG:2b4jpZ4l1gSCjc4PhfS=> MYj+NlAh|ryP NWjo[HRtTE2VTx?= NHrMUXBKSzVyPU[uOVI5KM7:TR?= NX62VGFGOTh{MEe3OFg>
LOVO NXLsPIY{[3m2b4TvfIlkcXS7IHHzd4F6 MnLBglIxKM7:TR?= Mm[xSG1UVw>? Ml7mTWM2OD17LkCxOUDPxE1? MlzFNVgzODd5NEi=
MCF7 M3nobYN6fG:2b4jpZ4l1gSCjc4PhfS=> Mkf2glIxKM7:TR?= NEHVZ2FFVVOR MX3JR|UxRTF5LkSwN{DPxE1? MV:xPFIxPzd2OB?=
LS174T NW\iN41yT3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MXfEUXNQ NETPdlVKSzVyPUGuNVYh|ryP M1zQSVE5PDd7MUG4
KB3-1 NVe3bpNR[3m2b4TvfIlkcXS7IHHzd4F6 NH:2S2pKSzVyPUCuOlgh|ryP NEnvPIsyQDd5MUmzNC=>
KBV-1 M4j0UIN6fG:2b4jpZ4l1gSCjc4PhfS=> M1j6[WlEPTB;NECg{txO Ml7BNVg4PzF7M{C=
KBH5.0 NYLlTnBS[3m2b4TvfIlkcXS7IHHzd4F6 M3fYPGlEPTB;Nz60JO69VQ>? NVfw[GpUOTh5N{G5N|A>
Hep G2 M3P1Nmdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 Ml3iglExKM7:TR?= NWiyTVAyTE2VTx?= MojJTWM2OD13Lkm0JO69VQ>? NUDnUZRzOTl5OU[5OVY>
Hep 3B MXvHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? M2HYOJ4yOCEQvF2= NGLaVYpFVVOR MnLBTWM2OD12LkezJO69VQ>? MVKxPVc6Pjl3Nh?=
Hep 2.2. MY\Hdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NG\4[FJ,OTBizszN NVL5TY5HTE2VTx?= M4G5W2lEPTB-MUCg{txO NYXRUFI5OTl5OU[5OVY>
A549 NFPOVJZkgXSxdH;4bYNqfHliYYPzZZk> NE[wd5VFVVOR NFzsO|ZKSzVyPUSuOlEh|ryP NFXtdXMzODN5MUG4Ny=>
MDA-MB-435 MW\jfZRwfG:6aXPpeJkh[XO|YYm= NXuyeoF7TE2VTx?= NI\HV2hKSzVyPUGuNVQh|ryP MnH2NlA{PzFzOEO=
LOVO MYrjfZRwfG:6aXPpeJkh[XO|YYm= MkH2SG1UVw>? Ml2wTWM2OD12Lkm5JO69VQ>? NXvzZZBZOjB|N{GxPFM>
MDA-MB-435 NH\lU2hkgXSxdH;4bYNqfHliYYPzZZk> NHT2XYVFVVOR M1v3cWlEPTB;MUeg{txO NUfT[XllOjB7NEK0PVA>
NCI60 NEDQOmJIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MWDEUXNQ M2DZ[mdKPTB;MUSuNVI2PCEQvF2= MnLLNlExOzV|M{S=
H460 Mn\hZ5l1d3SxeHnjbZR6KGG|c3H5 MljOSG1UVw>? MlOyTWM2OD1yLkCxOUDPxE1? M4fG[FIyOzRzNke0
PC-3 MUPjfZRwfG:6aXPpeJkh[XO|YYm= M2rYemROW09? MXfJR|UxRTBwMkKg{txO NFnRVWwzOTN2MU[3OC=>
HT29 MUDjfZRwfG:6aXPpeJkh[XO|YYm= NXL1N2tGTE2VTx?= Mn33TWM2OD1yLkCwOEDPxE1? MVuyNVM1OTZ5NB?=
SK-MEL-2 MUjjfZRwfG:6aXPpeJkh[XO|YYm= NVfDSGRQTE2VTx?= MYDJR|UxRTBwMTFOwG0> MUmyNVM1OTZ5NB?=
A375 MVnjfZRwfG:6aXPpeJkh[XO|YYm= NGrKc2FFVVOR MY\JR|UxRTBwMEC0JO69VQ>? MnH5NlE{PDF4N{S=
Malme-3M M2XPR4N6fG:2b4jpZ4l1gSCjc4PhfS=> M{TaU2ROW09? NXfzRplFUUN3ME2wMlIh|ryP M17jTlIyOzRzNke0
DU 145 NXjQUIhO[3m2b4TvfIlkcXS7IHHzd4F6 NIjxfFJFVVOR NV\pdFVwUUN3ME2wMlIh|ryP MUOyNVM1OTZ5NB?=
LNCaP NHTuTotkgXSxdH;4bYNqfHliYYPzZZk> MnvsSG1UVw>? NHfYOG9KSzVyPUCuNFA6KM7:TR?= MXWyNVM1OTZ5NB?=
IGROV-1 M3qwPYN6fG:2b4jpZ4l1gSCjc4PhfS=> MVHEUXNQ M2XiWmlEPTB;MD6wN{DPxE1? NY\nfnp{OjF|NEG2O|Q>
KB NUPzWZpJ[3m2b4TvfIlkcXS7IHHzd4F6 NHXaUYt,OjBizszN NUHjdGxuTE2VTx?= M3P0bmlEPTB;OT64N{DPxE1? NYrrboVQOjJyN{myOVQ>
KB-vin NHrVUXVkgXSxdH;4bYNqfHliYYPzZZk> MkDUglIxKM7:TR?= NFfwV2RFVVOR NVLrbo97UUN3ME6yNEDPxE1? NFv4bZkzOjB5OUK1OC=>

... 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]

- Collapse
  • 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]

- Collapse
  • Animal Models: Female nude mice with COLO 320 and WiDr xenografts
  • 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 Insoluble
Ethanol Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
30% propylene glycol, 5% Tween 80, 65% D5W
For best results, use promptly after mixing.
30 mg/mL

* 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 (+)-Irinotecan
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
NCT04866641 Not yet recruiting Drug: T-1201 Injection 100 mg Kit Advanced Solid Tumor Taivex Therapeutics Corporation July 5 2021 Phase 1
NCT04617522 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced or Metastatic Solid Tumor|Liver Failure Gilead Sciences April 6 2021 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID