Name: Irinotecan (CPT-11)
Brand: Selleck Chemicals
SKU: S1198
Rating: 5 (56 reviews)

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Kvalitetskontroll (Quality Control)

Batch: Renhet: 99.99%

99.99

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

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Cellinjer	Analystyp	Koncentration	Formulering	Aktivitetsbeskrivning
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
Klicka för att visa mer experimentella data för cellinjer

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Molekylvikt	586.68	Formel	C₃₃H₃₈N₄O₆	Lagring (från mottagningsdatumet)	3 år-20°Cpulver
CAS-nr	97682-44-5	Ladda ner SDF		Lagring av stamlösningar	1 år-80°Ci lösningsmedel 1 månad-20°Ci lösningsmedel
Synonymer	(+)-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

Löslighet (Solubility)

In vitro
Batch:

DMSO : 25 mg/mL (42.61 mM)
(Fuktkontaminerad DMSO kan minska lösligheten. Använd färk, vattenfri DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritetsräknare

Massa	Koncentration	Volym	Molekylvikt
=	×	×

Utspädningsräknare Molekylviktsräknare

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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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 Validerad av Selleck-laboratorier. Om du behöver justeringar av denna formulering, kontakta vårt säljteam för skräddarsydd testning.	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-formuleringsräknare (Klar lösning)

Steg 1: Ange information nedan (Rekommenderas: Ett extra djur för att ta hänsyn till förluster under experimentet)

Dosering: mg/kg Djurens medelvikt: g Doseringsvolym per djur:μL Antal djur:

Steg 2: Ange in vivo-formuleringen (Detta är endast räknaren, inte formuleringen. Vänligen kontakta oss först om det inte finns någon in vivo-formulering i löslighetsavsnittet.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Beräkningsresultat:

Arbetskoncentration: mg/ml;

Metod för att bereda DMSO-stamlösning: mg substans förlöst i μL DMSO ( Stamlösningskoncentration mg/mL, Vänligen kontakta oss först om koncentrationen överskrider DMSO-lösligheten för denna batch av substansen. )

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedanμL PEG300, blanda och klarna, tillsätt sedanμL Tween 80, blanda och klarna, tillsätt sedan μL ddH₂O, blanda och klarna.

Metod för att bereda in vivo-formulering: Ta μL DMSO stamlösning, tillsätt sedan μL Majsolja, blanda och klarna.

Obs: 1. Se till att vätskan är klar innan du tillsätter nästa lösningsmedel.
2. Se till att tillsätta lösningsmedlet/lösningsmedlen i ordning. Du måste se till att lösningen som erhålls i föregående tillsats är en klar lösning innan du fortsätter att tillsätta nästa lösningsmedel. Fysiska metoder som vortex, ultraljud eller varmt vattenbad kan användas för att underlätta upplösningen.

Verkningsmekanism (Mechanism of Action)

Egenskaper	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.
Referenser	[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/

Klinisk prövningsinformation (Clinical Trial Information)

(data från https://clinicaltrials.gov, uppdaterad den 2024-05-22)

NCT-nummer	Rekrytering	Tillstånd	Sponsor/Samarbetspartners	Startdatum	Faser
NCT05854498	Recruiting	Metastatic Colorectal Cancer	University of Wisconsin Madison\|Ipsen	October 13 2023	Phase 2
NCT05732129	Not yet recruiting	Homologous Recombination Deficiency Alterations Metastatic Colorectal Cancer	Fudan University	March 1 2023	Phase 2
NCT05731518	Recruiting	Small Cell Lung Cancer	Biocity Biopharmaceutics Co. Ltd.	February 23 2023	Phase 1\|Phase 2
NCT06003998	Recruiting	Colorectal Cancer\|Peritoneal Metastases	Catharina Ziekenhuis Eindhoven	December 27 2022	Phase 2
NCT05277766	Recruiting	Peritoneal Carcinomatosis\|Peritoneal Metastases\|Colorectal Cancer\|Small Bowel Cancer\|Appendix Cancer\|Gastric Cancer\|Pancreatic Cancer\|Bile Duct Cancer	University Hospital Ghent\|Kom Op Tegen Kanker\|University Ghent	November 21 2022	Phase 1
NCT05379790	Recruiting	Gastric Cancer\|Peritoneal Metastases	Erasmus Medical Center	May 25 2022	Phase 1

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-hämmare

Molekylvikt: 586.68

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Klinisk prövningsinformation (Clinical Trial Information)

Irinotecan (CPT-11) Topoisomerase I-hämmare

Molekylvikt: 586.68

Kvalitetskontroll (Quality Control)

Cellodling, behandling & arbetskoncentration (Cell Culture, Treatment & Working Concentration)

Kemisk information, lagring & stabilitet (Chemical Information, Storage & Stability)

Löslighet (Solubility)

Molaritetsräknare

In vivo-formuleringsräknare (Klar lösning)

Verkningsmekanism (Mechanism of Action)

Klinisk prövningsinformation (Clinical Trial Information)

Cellodling, behandling & arbetskoncentration
(Cell Culture, Treatment & Working Concentration)