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Irinotecan Hydrochloride Topoisomerase I Inhibitor

Cat.No.S5026

Irinotecan (CPT-11, (+)-Irinotecan) hydrochloride is an inhibitor of Topoisomerase I (Topo I) that exhibits cytotoxicity in LoVo cells and HT-29 cells with IC50 of 15.8 μM and 5.17 μM, respectively.
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Quality Control

Batch: Purity: 99.99%
99.99

Solubility

In vitro
Batch:

DMSO : 100 mg/mL (160.47 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

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In vivo
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Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
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Chemical Information, Storage & Stability

Molecular Weight 623.14 Formula

C33H39ClN4O6

Storage (From the date of receipt) 3 years -20°C powder
CAS No. 100286-90-6 -- Storage of Stock Solutions

Synonyms CPT-11 hydrochloride, (+)-Irinotecan hydrochloride SMILES Cl.CCC1=C2CN3C(=O)C4=C(C=C3C2=NC5=C1C=C(OC(=O)N6CCC(CC6)N7CCCCC7)C=C5)C(O)(CC)C(=O)OC4

Read more about storage stability stock solution CAS number SMILES

Mechanism of Action

Targets/IC50/Ki
Topo I
cytotoxicity in HT-29 cells
(Cell-based assay)
5.17 μM
cytotoxicity in LoVo cells
(Cell-based assay)
15.8 μM
In vitro

The combination of gefitinib and irinotecan has a significant synergistic effect on the proliferation and migration of MDA-MB-231 cells.

In vivo

The combination of gefitinib and irinotecan has a significant synergistic effect in the treatment of TNBC subtype cells in xenograft model.

References

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2026-06-18)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06365008 NOT_YET_RECRUITING
Unresectable/Metastatic Gastric Cancer
Sun Yat-Sen Memorial Hospital of Sun Yat-Sen University
2026-06 PHASE2
NCT07521605 NOT_YET_RECRUITING
Rectal Cancer Patients
Guangdong Provincial People's Hospital
2026-05-20 PHASE2
NCT07381764 NOT_YET_RECRUITING
Metastatic Colorectal Cancer (CRC)
Gruppo Oncologico Italia Meridionale
2026-03-30 PHASE2
NCT07549321 RECRUITING
High-Risk Neuroblastoma
Renaissance Pharma Ltd.
2026-03-30 PHASE2; PHASE3
NCT07585279 NOT_YET_RECRUITING
Metastatic Colorectal Cancer (CRC); Liposomal Irinotecan; Second-Line
Hebei Medical University Fourth Hospital
2026-05-20 PHASE2; PHASE3
NCT06401330 RECRUITING
Stage I Mixed Cell Type Kidney Wilms Tumor; Stage II Mixed Cell Type Kidney Wilms Tumor; Stage III Mixed Cell Type Kidney Wilms Tumor; Stage IV Mixed Cell Type Kidney Wilms Tumor
Children's Oncology Group
2025-04-15 PHASE3

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