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Chemical Structure| 136572-09-3 Chemical Structure| 136572-09-3

Structure of Irinotecan HCl Trihydrate
CAS No.: 136572-09-3

Chemical Structure| 136572-09-3

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Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate) is a topoisomerase I inhibitor with antitumor activity.

Synonyms: CPT-11 hydrochloride trihydrate; Irinotecan(hydrochloride hydrate); CPT-11 HCl Trihydrate

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Product Details of Irinotecan HCl Trihydrate

CAS No. :136572-09-3
Formula : C33H45ClN4O9
M.W : 677.18
SMILES Code : O=C(N1CCC(N2CCCCC2)CC1)OC3=CC=C4N=C5C(CN6C(C(COC([C@@]7(CC)O)=O)=C7C=C65)=O)=C(CC)C4=C3.[H]Cl.[H]O[H].[H]O[H].[H]O[H]
Synonyms :
CPT-11 hydrochloride trihydrate; Irinotecan(hydrochloride hydrate); CPT-11 HCl Trihydrate
MDL No. :MFCD01765731
InChI Key :KLEAIHJJLUAXIQ-JDRGBKBRSA-N
Pubchem ID :60837

Safety of Irinotecan HCl Trihydrate

GHS Pictogram:
Signal Word:Danger
Hazard Statements:H301
Precautionary Statements:P501-P270-P264-P301+P310+P330-P405
Class:6.1
UN#:2811
Packing Group:

Related Pathways of Irinotecan HCl Trihydrate

DNA

Isoform Comparison

Biological Activity

Description
Irinotecan hydrochloride trihydrate ((+)-Irinotecan hydrochloride trihydrate), a potent topoisomerase I inhibitor, exhibits antitumor properties[1].
Target
  • Topo I

In Vitro:

Cell Line
Concentration Treated Time Description References
C2C12 cells 50 μg/mL 1 h To evaluate the effect of SR12343 on FOLFIRI-induced markers of cellular senescence. SR12343 significantly reduced the expression levels of p53, p21, Tnfa, and Il1a. PMC10906225
HT-29 20 µM 1.5 h To investigate the effects of irinotecan alone or in combination with 5-FU on the growth, metabolic activity, proliferation, and clonogenic survival of HT-29 cells. Results showed that irinotecan alone or in combination with 5-FU significantly inhibited the growth, metabolic activity, and clonogenic survival of HT-29 cells, and significantly increased the radiosensitivity of tumor cells. PMC10299222
EC-109 0–125 μM 48 h To evaluate the inhibitory effect of Irinotecan on the proliferation of EC-109 cells, the results showed that Irinotecan significantly inhibited cell proliferation at micromolar concentrations. PMC5981453
KYSE-450 0–125 μM 48 h To evaluate the inhibitory effect of Irinotecan on the proliferation of KYSE-450 cells, the results showed that Irinotecan significantly inhibited cell proliferation at micromolar concentrations. PMC5981453
LAN-1 100, 10, 1 nM 72 h To study the cytotoxicity of SN-38, results showed that all SN-38-loaded NPs retained activity in the low nanomolar concentration range PMC5564453
HeLa 100, 10, 1 nM 72 h To study the cytotoxicity of SN-38, results showed that all SN-38-loaded NPs retained activity in the low nanomolar concentration range PMC5564453
293T cells 10 µM 24 h Increased the proportion of cells in S and G2/M phases, promoting CRISPR/Cas9-mediated homology-directed repair (HDR) efficiency PMC10676593
BHK-21 cells 1-10 µM 48 h Dose-dependent increase in dsDNA and ssODN-mediated knock-in (KI) efficiency PMC10676593
pig fetal fibroblasts (PFFs) 1-10 µM 48 h Dose-dependent increase in knock-in (KI) efficiency PMC10676593
SW480 cells 10 μM 48 h To evaluate the effect of Irinotecan on SW480 cells, results showed decreased cell viability after Irinotecan treatment. PMC6947904
U87 cells 10 μM 72 h Irinotecan showed anti-GBM activity in U87 cells with an IC50 value lower than other compounds. PMC3898565
SK72 cells 30 μM Irinotecan showed anti-GBM activity in SK72 cells with an IC50 value of 30 μM. PMC3898565

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Mice C57BL/6J mice Intraperitoneal injection 24 mg/kg 3 times per week for 9 weeks To evaluate the effect of FOLFIRI on, lean mass, and fat mass in mice. FOLFIRI significantly reduced, lean mass, and fat mass, and increased the expression of markers of cellular senescence. PMC10906225
Mice C57BL/6 mice Intravenous injection 40 mg/kg Every 3 or 4 days for 4 to 6 administrations In the orthotopic MC38 tumor model, the Ir-silicasome demonstrated improved pharmacokinetics and tumor drug content compared to free drug and Onivyde?, significantly enhancing therapeutic efficacy, prolonging survival, and reducing bone marrow and gastrointestinal toxicity. PMC6554030
BALB/c nude mice subcutaneous xenograft model intraperitoneal injection 5 mg/kg twice per week, for approximately 50 days To study the role of eIF3a in irinotecan sensitivity in vivo, it was found that eIF3a silencing significantly increased tumor resistance to irinotecan. PMC9055905
NOD/SCID mice ESCC cell line xenograft models Intraperitoneal injection 8 mg/kg Twice a week for 3 weeks To evaluate the antitumor effect of Irinotecan in ESCC xenograft models, the results showed that Irinotecan significantly inhibited tumor growth, but the effect was inferior to Gimatecan. PMC5981453
pig pig embryos embryo injection 5 µM single injection, incubated for 6 days Significantly increased knock-in (KI) frequency in pig embryos without impairing embryo development PMC10676593
Nude mice U87 cell subcutaneous xenograft model Intraperitoneal injection 0.5 mg/kg Once daily for 5 days, followed by 2 days off The combination of irinotecan with pitavastatin significantly inhibited tumor growth with lower toxicity. PMC3898565

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00483834 Colorectal Cancer Phase 2 Completed - Canada, Ontario ... More >> Princess Margaret Hospital Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT03245450 Refractory or Recurrent Solid ... More >>Tumors Rhabdomyosarcoma Non-Rhabdomyosarcoma Soft Tissue Sarcoma Ewing Sarcoma Less << Phase 1 Phase 2 Recruiting June 30, 2021 Germany ... More >> Uniklinik RWTH Aachen Kinderklinik Recruiting Aachen, Germany Charite Virchow Kinderklinik - CC17 Recruiting Berlin, Germany Uniklinik Essen AoR Kinderklinik Recruiting Essen, Germany Klinik fur Kinder und Jugendmed - KKJM Recruiting Frankfurt, Germany Uniklinik Freiburg Kindermedizin Klinik IV Recruiting Freiburg, Germany Uniklinik Gottingen Kindermedizin Recruiting Gottingen, Germany Kinderklinik Muenchen Schwabing Not yet recruiting Muenchen, Germany Less <<
NCT02015754 Colorectal Cancer Phase 2 Completed - United States, Maryland ... More >> The Johns Hopkins Hospital Baltimore, Maryland, United States, 21287 Less <<
NCT03175016 Colon Cancer Liver Metastasis Phase 2 Phase 3 Recruiting December 2019 China, Tianjin ... More >> Tianjin Medical University Cancer Institute and Hospital Recruiting Tianjin, Tianjin, China, 300060 Contact: Zhi Guo, MD    13920076145    cjr.guozhi@vip.163.com    Contact: Xueling Yang, MD    15620930669    yxueling123@163.com    Sub-Investigator: Wenge Xing Less <<
NCT00540943 Neoplasms, Colorectal Phase 1 Completed - France ... More >> GSK Investigational Site Saint Herblain, France, 44805 GSK Investigational Site Toulouse, France, 31052 Less <<
NCT00003225 Colorectal Cancer Phase 1 Phase 2 Completed - United States, California ... More >> Jonsson Comprehensive Cancer Center, UCLA Los Angeles, California, United States, 90095-1781 Wilshire Oncology Medical Group, Inc. Rancho Cucamonga, California, United States, 91730 Less <<
NCT01494506 Metastatic Pancreatic Cancer Phase 3 Completed - -
NCT00393094 High-Grade Gliomas Phase 2 Terminated(Terminated due to t... More >>he limitations of accrual.) Less << - United States, Maryland ... More >> National Institutes of Health Clinical Center, 9000 Rockville Pike Bethesda, Maryland, United States, 20892 Less <<
NCT01494506 - Completed - -
NCT02015754 - Completed - -
NCT00004919 Unspecified Childhood Solid Tu... More >>mor, Protocol Specific Less << Phase 1 Completed - United States, California ... More >> COG Phase I Consortium Arcadia, California, United States, 91006-3776 Less <<
NCT00393094 - Terminated(Terminated due to t... More >>he limitations of accrual.) Less << - -
NCT00693719 Breast Cancer Phase 2 Completed - United States, Arizona ... More >> Arizona Cancer Center at University of Arizona Health Sciences Center Tucson, Arizona, United States, 85724-5024 Less <<
NCT00160875 Esophageal Cancer Phase 2 Phase 3 Completed - Canada, Ontario ... More >> University Health Network Toronto, Ontario, Canada, M5G 2M9 Less <<
NCT00693719 - Completed - -

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

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1.48mL

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0.15mL

7.38mL

1.48mL

0.74mL

14.77mL

2.95mL

1.48mL

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