Name: Irinotecan (CPT-11)
Brand: Selleck Chemicals
SKU: S1198
Rating: 5 (59 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.99%

99.99

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN DNA/RNA Synthesis PPAR Sirtuin Casein Kinase eIF
Overige Topoisomerase Inhibitoren	Camptothecin (CPT) Betulinic acid (S)-10-Hydroxycamptothecin Beta-Lapachone Ellagic acid Amonafide Voreloxin (SNS-595) hydrochloride Hydroxy Camptothecine Cu(II)-Elesclomol 7-Ethylcamptothecin

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen	Assaytype	Concentratie	Formulering	Activiteitsbeschrijving
HCT116	cytotoxicity assay	10 μM	DMSO	ID50=540 nM
VM46	cytotoxicity assay	10 μM	DMSO	ID50=220 nM
MCF-7ADR	cytotoxicity assay	10 μM	DMSO	ID50>500 nM
L1210	cytotoxicity assay			IC50=1.2 µM
RPMI8402	cytotoxicity assay	100 μM		IC50=570 nM
A-549	cytotoxicity assay	~20 μM	DMSO	IC50=6.528 μM
LOVO	cytotoxicity assay	~20 μM	DMSO	IC50=9.015 μM
MCF7	cytotoxicity assay	~20 μM	DMSO	IC50=17.403 μM
LS174T	Growth inhibitory assay		DMSO	IC50=1.16 μM
KB3-1	cytotoxicity assay			IC50=0.68 μM
KBV-1	cytotoxicity assay			IC50=40 μM
KBH5.0	cytotoxicity assay			IC50=7.4 μM
Hep G2	Growth inhibitory assay	~10 μM	DMSO	IC50=5.94 μM
Hep 3B	Growth inhibitory assay	~10 μM	DMSO	IC50=4.73 μM
Hep 2.2.	Growth inhibitory assay	~10 μM	DMSO	IC50>10 μM
A549	cytotoxicity assay		DMSO	IC50=4.61 μM
MDA-MB-435	cytotoxicity assay		DMSO	IC50=1.14 μM
LOVO	cytotoxicity assay		DMSO	IC50=4.99 μM
MDA-MB-435	cytotoxicity assay		DMSO	IC50=17 μM
NCI60	Growth inhibitory assay		DMSO	GI50=14.1254 μM
H460	cytotoxicity assay		DMSO	IC50=0.015 μM
PC-3	cytotoxicity assay		DMSO	IC50=0.22 μM
HT29	cytotoxicity assay		DMSO	IC50=0.004 μM
SK-MEL-2	cytotoxicity assay		DMSO	IC50=0.1 μM
A375	cytotoxicity assay		DMSO	IC50=0.004 μM
Malme-3M	cytotoxicity assay		DMSO	IC50=0.2 μM
DU 145	cytotoxicity assay		DMSO	IC50=0.2 μM
LNCaP	cytotoxicity assay		DMSO	IC50=0.009 μM
IGROV-1	cytotoxicity assay		DMSO	IC50=0.03 μM
KB	cytotoxicity assay	~20 μM	DMSO	IC50=9.83 μM
KB-vin	cytotoxicity assay	~20 μM	DMSO	IC50>20 μM
Klik om meer experimentele gegevens over de cellijn te bekijken

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Moleculair gewicht	586.68	Formule	C₃₃H₃₈N₄O₆	Opslag (Vanaf de ontvangstdatum)	3 jaar-20°Cpoeder
CAS-nr.	97682-44-5	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
Synoniemen	(+)-Irinotecan,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

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 25 mg/mL (42.61 mM)
(Met vocht verontreinigde DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa	Concentratie	Volume	Moleculair gewicht
=	×	×

Verdunningscalculator Moleculair gewicht calculator

In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	7%DMSO 1 93%Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	2.100mg/ml (3.58mM)	Taking the 1 mL working solution as an example, add 70 μL of 30 mg/ml clear DMSO stock solution to 930 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	6.000mg/ml (10.23mM)	Taking the 1 mL working solution as an example, add 50 μL of 120 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Clear solution	5% DMSO 1 95% Corn oil Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.500mg/ml (0.85mM)	Taking the 1 mL working solution as an example, add 50 μL of 10 mg/ml clear DMSO stock solution to 950 μL of corn oil and mix evenly. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formuleringscalculator (Heldere oplossing)

Stap 1: Voer de onderstaande informatie in (Aanbevolen: Een extra dier voor het geval van verlies tijdens het experiment)

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

Stap 2: Voer de in vivo formulering in (Dit is alleen de calculator, geen formulering. Neem eerst contact met ons op als er geen in vivo formulering is in het gedeelte Oplosbaarheid.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

Methode voor het bereiden van DMSO-mastervloeistof: mg geneesmiddel vooraf opgelost in μL DMSO ( Concentratie mastervloeistof mg/mL, Neem eerst contact met ons op als de concentratie de DMSO-oplosbaarheid van de partij geneesmiddel overschrijdt. )

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toeμL PEG300, mengen en helder maken, voeg vervolgens toeμL Tween 80, mengen en helder maken, voeg vervolgens toe μL ddH₂O, mengen en helder maken.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO mastervloeistof, voeg vervolgens toe μL Maïsolie, mengen en helder maken.

Opmerking: 1. Zorg ervoor dat de vloeistof helder is voordat u het volgende oplosmiddel toevoegt.
2. Zorg ervoor dat u het/de oplosmiddel(en) in de juiste volgorde toevoegt. U moet ervoor zorgen dat de verkregen oplossing, bij de vorige toevoeging, een heldere oplossing is voordat u verdergaat met het toevoegen van het volgende oplosmiddel. Fysische methoden zoals vortexen, echografie of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (Mechanism of Action)

Kenmerken	Irinotecan is a prodrug that is used to treat metastatic colorectal cancer.
Targets/IC₅₀/Ki	Topo I (LoVo, HT-29 cells)
In vitro	Irinotecan is activated to SN-38 by carboxylesterases to become able to interact with its target, topoisomerase I. This compound 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 this chemical is markedly different, reaching consistently higher levels in HT-29 cells than in LoVo cells. The lactone E-ring of this compound 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 this agent to SN-38. At equal concentrations of this drug and SN-38 glucuronide, the rate of beta-glucuronidase-mediated SN-38 production is higher than that formed from this compound in both tumour and normal tissue. It is also converted to SN-38 in intestines, plasma and tumor tissues. This agent is significantly more active in SCLC than in NSCLC cell lines, whereas no significant difference between histological types is observed with SN-38.
In vivo	In COLO 320 xenografts, Irinotecan induces a maximum growth inhibition of 92%. A single dose of this compound 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.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/11914913/ [2] https://pubmed.ncbi.nlm.nih.gov/16842384/ [3] https://pubmed.ncbi.nlm.nih.gov/15182436/ [4] https://pubmed.ncbi.nlm.nih.gov/9649129/ [5] https://pubmed.ncbi.nlm.nih.gov/9033637/ [6] https://pubmed.ncbi.nlm.nih.gov/21046105/ [7] https://pubmed.ncbi.nlm.nih.gov/16317751/

Informatie klinische proef (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-06-18)

NCT-nummer	Rekrutering	Aandoeningen	Sponsor/Medewerkers	Startdatum	Fasen
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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Irinotecan (CPT-11) Topoisomerase I-remmer

Moleculair gewicht: 586.68

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

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In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie klinische proef (Clinical Trial Information)

Irinotecan (CPT-11) Topoisomerase I-remmer

Moleculair gewicht: 586.68

Kwaliteitscontrole (Quality Control)

Celkweek, behandeling & werkconcentratie (Cell Culture, Treatment & Working Concentration)

Chemische informatie, Opslag en Stabiliteit (Chemical Information, Storage & Stability)

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo Formuleringscalculator (Heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie klinische proef (Clinical Trial Information)

Celkweek, behandeling & werkconcentratie
(Cell Culture, Treatment & Working Concentration)