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

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Control de calidad (Quality Control)

Lote: Pureza: 99.99%

99.99

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

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Líneas celulares	Tipo de ensayo	Concentración	Formulación	Descripción de la actividad
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
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular	586.68	Fórmula	C₃₃H₃₈N₄O₆	Almacenamiento (Desde la fecha de recepción)	3 años-20°Cpolvo
Nº CAS	97682-44-5	Descargar SDF		Almacenamiento de soluciones madre	1 año-80°Cen disolvente 1 mes-20°Cen disolvente
Sinónimos	(+)-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

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 25 mg/mL (42.61 mM)
(El DMSO contaminado con humedad puede reducir la solubilidad. Usar DMSO fresco y anhidro.)

Water : Insoluble

Ethanol : Insoluble

Calculadora de Molaridad

Masa	Concentración	Volumen	Peso molecular
=	×	×

Calculadora de Dilución Calculadora de Peso Molecular

In vivo Lote:
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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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 Validado por los laboratorios Selleck. Si necesita ajustes en esta formulación, contacte con nuestro equipo de ventas para pruebas personalizadas.	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.

Calculadora de formulación in vivo (Solución clara)

Paso 1: Introduzca la información a continuación (Recomendado: Un animal adicional para tener en cuenta la pérdida durante el experimento)

Dosis: mg/kg Peso promedio de los animales: g Volumen de dosificación por animal:μL Número de animales:

Paso 2: Introduzca la formulación in vivo (Esto es solo la calculadora, no la formulación. Por favor, contáctenos primero si no hay una formulación in vivo en la sección de Solubilidad.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Resultados del cálculo:

Concentración de trabajo: mg/ml;

Método para preparar el líquido maestro de DMSO: mg fármaco predissuelto en μL DMSO ( Concentración del líquido maestro mg/mL, Por favor, contáctenos primero si la concentración excede la solubilidad del DMSO del lote del fármaco. )

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadirμL PEG300, mezclar y clarificar, luego añadirμL Tween 80, mezclar y clarificar, luego añadir μL ddH₂O, mezclar y clarificar.

Método para preparar la formulación in vivo: Tomar μL DMSO líquido maestro, luego añadir μL Aceite de maíz, mezclar y clarificar.

Nota: 1. Por favor, asegúrese de que el líquido esté claro antes de añadir el siguiente disolvente.
2. Asegúrese de añadir el (los) disolvente(s) en orden. Debe asegurarse de que la solución obtenida, en la adición anterior, sea una solución clara antes de proceder a añadir el siguiente disolvente. Se pueden utilizar métodos físicos como el vórtice, el ultrasonido o el baño de agua caliente para ayudar a la disolución.

Mecanismo de acción (Mechanism of Action)

Características	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.
Referencias	[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/

Información del ensayo clínico (Clinical Trial Information)

(datos de https://clinicaltrials.gov, actualizado el 2024-05-22)

Número NCT	Reclutamiento	Condiciones	Patrocinador/Colaboradores	Fecha de inicio	Fases
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 Inhibitor

Peso molecular: 586.68

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

Irinotecan (CPT-11) Topoisomerase I Inhibitor

Peso molecular: 586.68

Control de calidad (Quality Control)

Cultivo celular, tratamiento y concentración de trabajo (Cell Culture, Treatment & Working Concentration)

Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Solubilidad (Solubility)

Calculadora de Molaridad

Calculadora de formulación in vivo (Solución clara)

Mecanismo de acción (Mechanism of Action)

Información del ensayo clínico (Clinical Trial Information)

Cultivo celular, tratamiento y concentración de trabajo
(Cell Culture, Treatment & Working Concentration)