Irinotecan

For research use only.

Catalog No.S1198 Synonyms: CPT-11

2 publications

Irinotecan Chemical Structure

CAS No. 97682-44-5

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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10mM (1mL in DMSO) EUR 88 In stock
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Selleck's Irinotecan has been cited by 2 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 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 M3HFVoN6fG:2b4jpZ4l1gSCjc4PhfS=> M4fjOlExKM7:TR?= MY\EUXNQ MXPJSFUxRTV2MDDuUS=> NXzHe|ZvOTF7NkWzOlI>
VM46 MUDjfZRwfG:6aXPpeJkh[XO|YYm= Ml;vNVAh|ryP NIGxcIJFVVOR NEXJb3hKTDVyPUKyNEBvVQ>? MXSxNVk3PTN4Mh?=
MCF-7ADR MXjjfZRwfG:6aXPpeJkh[XO|YYm= NGexOGcyOCEQvF2= MYTEUXNQ M1n3RWlFPTB-NUCwJI5O NVPBUXlOOTF7NkWzOlI>
L1210 NYPYOVJl[3m2b4TvfIlkcXS7IHHzd4F6 MUTJR|UxRTFwMjFCuW0> NYrSb3B4OTh2NkmyNy=>
RPMI8402 NIHWe5dkgXSxdH;4bYNqfHliYYPzZZk> M1[zclExOCEQvF2= MV3JR|UxRTV5MDDuUS=> M1[2OlEzPzR5N{m4
A-549 M2\Fb4N6fG:2b4jpZ4l1gSCjc4PhfS=> M{O0TZ4zOCEQvF2= M{O3NmROW09? MWHJR|UxRTZwNUK4JO69VQ>? NH20cHIyQDJyN{e0PC=>
LOVO MkTBZ5l1d3SxeHnjbZR6KGG|c3H5 MWL+NlAh|ryP M1PrVGROW09? MkfJTWM2OD17LkCxOUDPxE1? MlT2NVgzODd5NEi=
MCF7 MYHjfZRwfG:6aXPpeJkh[XO|YYm= Ml3NglIxKM7:TR?= M2LibWROW09? NGi1c|RKSzVyPUG3MlQxOyEQvF2= M1;6[VE5OjB5N{S4
LS174T MlLnS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? NILM[HRFVVOR NXXhZ5ZvUUN3ME2xMlE3KM7:TR?= MkfsNVg1PzlzMUi=
KB3-1 NHH2dWlkgXSxdH;4bYNqfHliYYPzZZk> NXnTRmMyUUN3ME2wMlY5KM7:TR?= MmruNVg4PzF7M{C=
KBV-1 NFPqbXhkgXSxdH;4bYNqfHliYYPzZZk> M{jqfWlEPTB;NECg{txO NE\XPVUyQDd5MUmzNC=>
KBH5.0 M3zwc4N6fG:2b4jpZ4l1gSCjc4PhfS=> NHf0[ZdKSzVyPUeuOEDPxE1? NYX4NWxVOTh5N{G5N|A>
Hep G2 NEXINopIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MUD+NVAh|ryP MkjjSG1UVw>? MUTJR|UxRTVwOUSg{txO MmTQNVk4QTZ7NU[=
Hep 3B MlXUS5Jwf3SqIHnubIljcXSxcomgZZN{[Xl? MkmyglExKM7:TR?= MmjoSG1UVw>? M{\OdmlEPTB;ND63N{DPxE1? MV2xPVc6Pjl3Nh?=
Hep 2.2. NHu0SGhIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= NXuze4tthjFyIN88US=> MVvEUXNQ Ml32TWM2OD5zMDFOwG0> M1;MXlE6Pzl4OUW2
A549 NYmyUnJG[3m2b4TvfIlkcXS7IHHzd4F6 NGHNNlNFVVOR MnftTWM2OD12Lk[xJO69VQ>? MYOyNFM4OTF6Mx?=
MDA-MB-435 Mk\HZ5l1d3SxeHnjbZR6KGG|c3H5 NYHRNoszTE2VTx?= MnnKTWM2OD1zLkG0JO69VQ>? MkXaNlA{PzFzOEO=
LOVO M1TH[4N6fG:2b4jpZ4l1gSCjc4PhfS=> Mk[ySG1UVw>? M4nNbmlEPTB;ND65PUDPxE1? MYGyNFM4OTF6Mx?=
MDA-MB-435 MXPjfZRwfG:6aXPpeJkh[XO|YYm= MU\EUXNQ M2GxTWlEPTB;MUeg{txO NUHWV5pwOjB7NEK0PVA>
NCI60 MWTHdo94fGhiaX7obYJqfG:{eTDhd5NigQ>? NI\KSZNFVVOR MUHHTVUxRTF2LkGyOVQh|ryP M2jtU|IyODN3M{O0
H460 MXXjfZRwfG:6aXPpeJkh[XO|YYm= MluwSG1UVw>? M2C3PGlEPTB;MD6wNVUh|ryP M4S2RVIyOzRzNke0
PC-3 NXfsXmZq[3m2b4TvfIlkcXS7IHHzd4F6 Mn7zSG1UVw>? NX71ZXYzUUN3ME2wMlIzKM7:TR?= MoS3NlE{PDF4N{S=
HT29 NWPCeJhq[3m2b4TvfIlkcXS7IHHzd4F6 M1fIfGROW09? MmLLTWM2OD1yLkCwOEDPxE1? NHrHbFMzOTN2MU[3OC=>
SK-MEL-2 NXfWbW05[3m2b4TvfIlkcXS7IHHzd4F6 M1jITWROW09? MX3JR|UxRTBwMTFOwG0> MUeyNVM1OTZ5NB?=
A375 NIDGeoNkgXSxdH;4bYNqfHliYYPzZZk> MUXEUXNQ NFrPTXdKSzVyPUCuNFA1KM7:TR?= M1rMNlIyOzRzNke0
Malme-3M MWLjfZRwfG:6aXPpeJkh[XO|YYm= NFnXPG5FVVOR M2LQV2lEPTB;MD6yJO69VQ>? MX6yNVM1OTZ5NB?=
DU 145 M1LzSoN6fG:2b4jpZ4l1gSCjc4PhfS=> NVHJWVRCTE2VTx?= MoO2TWM2OD1yLkKg{txO NVjJe3ZbOjF|NEG2O|Q>
LNCaP MXPjfZRwfG:6aXPpeJkh[XO|YYm= NY\SdoFJTE2VTx?= NHfxeZJKSzVyPUCuNFA6KM7:TR?= NVL4U|lFOjF|NEG2O|Q>
IGROV-1 M1PTeoN6fG:2b4jpZ4l1gSCjc4PhfS=> NWDWWVVWTE2VTx?= MVrJR|UxRTBwMEOg{txO NGnDUpQzOTN2MU[3OC=>
KB NFu5fZZkgXSxdH;4bYNqfHliYYPzZZk> M1LoN54zOCEQvF2= M4PSfGROW09? MojTTWM2OD17LkizJO69VQ>? MY[yNlA4QTJ3NB?=
KB-vin NWXMZWF1[3m2b4TvfIlkcXS7IHHzd4F6 Ml;0glIxKM7:TR?= M1XlVWROW09? Mn36TWM2OD5{MDFOwG0> Mn\yNlIxPzl{NUS=

... 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 CPT-11
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
NCT04238819 Not yet recruiting Drug: Abemaciclib|Drug: Irinotecan|Drug: Temozolomide Relapsed Solid Tumor|Refractory Solid Tumor Eli Lilly and Company October 20 2020 Phase 1
NCT04158349 Recruiting Drug: Oxaliplatin|Drug: mFOLFIRI Colorectal Cancer|Appendiceal Cancer|Peritoneal Carcinoma University of Utah June 11 2020 Phase 1
NCT04164979 Recruiting Drug: Cabozantinib|Drug: Pembrolizumab Gastric Adenocarcinoma|GastroEsophageal Cancer University of California Irvine|Exelixis February 4 2020 Phase 2

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID