Irinotecan (CPT-11)

Catalog No.S1198 Synonyms: (+)-Irinotecan

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 23 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 NEfjdJBkgXSxdH;4bYNqfHliYYPzZZk> NVv0cWp[OTBizszN NWfrR2hzTE2VTx?= M1;YVWlFPTB;NUSwJI5O NXPWdo5MOTF7NkWzOlI>
VM46 Mli0Z5l1d3SxeHnjbZR6KGG|c3H5 NI[wd5YyOCEQvF2= M{GxcmROW09? MUnJSFUxRTJ{MDDuUS=> MoiyNVE6PjV|NkK=
MCF-7ADR NXjxc49b[3m2b4TvfIlkcXS7IHHzd4F6 MXmxNEDPxE1? M2rEcGROW09? M2Xle2lFPTB-NUCwJI5O MUKxNVk3PTN4Mh?=
L1210 NX\rOWk5[3m2b4TvfIlkcXS7IHHzd4F6 MlzxTWM2OD1zLkKgxtVO MkLtNVg1Pjl{Mx?=
RPMI8402 MkDCZ5l1d3SxeHnjbZR6KGG|c3H5 MXGxNFAh|ryP NIrm[|FKSzVyPUW3NEBvVQ>? NXTGWYl7OTJ5NEe3PVg>
A-549 MYDjfZRwfG:6aXPpeJkh[XO|YYm= M3v2ep4zOCEQvF2= M3vZVGROW09? NX\OPYR6UUN3ME22MlUzQCEQvF2= MoLINVgzODd5NEi=
LOVO Mm[2Z5l1d3SxeHnjbZR6KGG|c3H5 NHHDcnJ,OjBizszN MWDEUXNQ NYTpO2Z[UUN3ME25MlAyPSEQvF2= MVmxPFIxPzd2OB?=
MCF7 MYnjfZRwfG:6aXPpeJkh[XO|YYm= Mn\1glIxKM7:TR?= MojGSG1UVw>? M3nWUGlEPTB;MUeuOFA{KM7:TR?= MW[xPFIxPzd2OB?=
LS174T M3joTGdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 NVXCOFI{TE2VTx?= NVm1PG5RUUN3ME2xMlE3KM7:TR?= NGO1e4IyQDR5OUGxPC=>
KB3-1 Ml7VZ5l1d3SxeHnjbZR6KGG|c3H5 MkTYTWM2OD1yLk[4JO69VQ>? NWHOVlhPOTh5N{G5N|A>
KBV-1 M3LDc4N6fG:2b4jpZ4l1gSCjc4PhfS=> MkXMTWM2OD12MDFOwG0> M3fFTFE5PzdzOUOw
KBH5.0 M1;HOoN6fG:2b4jpZ4l1gSCjc4PhfS=> MVzJR|UxRTdwNDFOwG0> NE\RcIIyQDd5MUmzNC=>
Hep G2 NH\VXGZIem:5dHigbY5pcWKrdH;yfUBie3OjeR?= MYH+NVAh|ryP MYTEUXNQ NYPBU5ZGUUN3ME21Mlk1KM7:TR?= MnewNVk4QTZ7NU[=
Hep 3B NYTS[FA{T3Kxd4ToJIlvcGmkaYTvdpkh[XO|YYm= MVn+NVAh|ryP M2rwXWROW09? M1PZN2lEPTB;ND63N{DPxE1? MVWxPVc6Pjl3Nh?=
Hep 2.2. M1fNcWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MlXnglExKM7:TR?= MXzEUXNQ MkXxTWM2OD5zMDFOwG0> M1faZVE6Pzl4OUW2
A549 NWXxN5RJ[3m2b4TvfIlkcXS7IHHzd4F6 MlftSG1UVw>? M1TLVWlEPTB;ND62NUDPxE1? M{G4TlIxOzdzMUiz
MDA-MB-435 NE\S[mhkgXSxdH;4bYNqfHliYYPzZZk> MmK0SG1UVw>? MVnJR|UxRTFwMUSg{txO Mo\3NlA{PzFzOEO=
LOVO Mn3iZ5l1d3SxeHnjbZR6KGG|c3H5 NEHFPGZFVVOR NYLtc2Q6UUN3ME20Mlk6KM7:TR?= M2K5UlIxOzdzMUiz
MDA-MB-435 MnTDZ5l1d3SxeHnjbZR6KGG|c3H5 NUm0SXc6TE2VTx?= NXf4RmRRUUN3ME2xO{DPxE1? NFj6PGszODl2MkS5NC=>
NCI60 M1TBbWdzd3e2aDDpcohq[mm2b4L5JIF{e2G7 MX3EUXNQ NYDJd5duT0l3ME2xOE4yOjV2IN88US=> MUKyNVA{PTN|NB?=
H460 NFvxZpFkgXSxdH;4bYNqfHliYYPzZZk> NIe1cWZFVVOR NWG2dnRJUUN3ME2wMlAyPSEQvF2= MX2yNVM1OTZ5NB?=
PC-3 NYPtSnJ7[3m2b4TvfIlkcXS7IHHzd4F6 MkX6SG1UVw>? MX7JR|UxRTBwMkKg{txO NVexWoIzOjF|NEG2O|Q>
HT29 NVfiTWZ7[3m2b4TvfIlkcXS7IHHzd4F6 Mm[wSG1UVw>? NUG5dml3UUN3ME2wMlAxPCEQvF2= NYD4fYJMOjF|NEG2O|Q>
SK-MEL-2 NEnyfFRkgXSxdH;4bYNqfHliYYPzZZk> MW\EUXNQ M1e0c2lEPTB;MD6xJO69VQ>? MnnhNlE{PDF4N{S=
A375 NYCwV4V4[3m2b4TvfIlkcXS7IHHzd4F6 M1XkW2ROW09? NFz6dHRKSzVyPUCuNFA1KM7:TR?= NHT0VWozOTN2MU[3OC=>
Malme-3M MlPDZ5l1d3SxeHnjbZR6KGG|c3H5 Mn\VSG1UVw>? MkTNTWM2OD1yLkKg{txO Mn\rNlE{PDF4N{S=
DU 145 MkHKZ5l1d3SxeHnjbZR6KGG|c3H5 NFTJeIRFVVOR M4LwRmlEPTB;MD6yJO69VQ>? M{nXUVIyOzRzNke0
LNCaP MWHjfZRwfG:6aXPpeJkh[XO|YYm= MXrEUXNQ MlT1TWM2OD1yLkCwPUDPxE1? NUjHbFdtOjF|NEG2O|Q>
IGROV-1 M2jXWoN6fG:2b4jpZ4l1gSCjc4PhfS=> NH;sVnhFVVOR M2DCcmlEPTB;MD6wN{DPxE1? NFXJXJczOTN2MU[3OC=>
KB M4W0T4N6fG:2b4jpZ4l1gSCjc4PhfS=> NUj0e5cyhjJyIN88US=> NFfkRWlFVVOR NGj2XWxKSzVyPUmuPFMh|ryP MmTJNlIxPzl{NUS=
KB-vin NV6xfIxI[3m2b4TvfIlkcXS7IHHzd4F6 NWexbYg6hjJyIN88US=> MXzEUXNQ M2TGOGlEPTB-MkCg{txO M3;P[lIzODd7MkW0
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

DMSO 7 mg/mL
(11.93 mM)
Water Insoluble
Ethanol Insoluble

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
NCT05101096 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced Solid Tumors or Triple-negative Breast Cancer Gilead Sciences October 20 2021 Phase 1|Phase 2
NCT04866641 Recruiting Drug: T-1201 Injection 100 mg Kit Advanced Solid Tumor Taivex Therapeutics Corporation June 24 2021 Phase 1
NCT04617522 Recruiting Drug: Sacituzumab Govitecan-hziy Advanced or Metastatic Solid Tumor|Liver Failure Gilead Sciences April 6 2021 Phase 1

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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