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Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibidor

Cat. No.: S1305

Mercaptopurine (6-MP) es un agente antileucémico y un fármaco inmunosupresor ampliamente utilizado que inhibe la síntesis de novo de purinas a través de la incorporación de metabolitos de la tiopurina metiltransferasa en el ADN y el ARN.
Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibidor Chemical Structure

Estructura química

Peso molecular: 152.18

Saltar a

Control de calidad (Quality Control)

Lote: Pureza: 99.97%
99.97

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

Líneas celulares Tipo de ensayo Concentración Tiempo de incubación Formulación Descripción de la actividad PMID
L1210 leukemia cells Function assay Inhibitory concentration on multidrug-resistant L1210 leukemia cells, IC50=0.024 μM
MT4 cells Proliferation assay Antiproliferative activity against human MT4 cells by MTT assay, IC50=0.1 μM
human CCRF-CEM cells Proliferation assay Antiproliferative activity against human CCRF-CEM cells by MTT assay, IC50=1 μM
human CCRF-SB cells Proliferation assay Antiproliferative activity against human CCRF-SB cells by MTT assay, IC50=1 μM
human SK-MEL-28 cells Proliferation assay Antiproliferative activity against human SK-MEL-28 cells by MTT assay, IC50=15 μM
human MCF7 cells Proliferation assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50=3 μM
human HepG2 cells Proliferation assay Antiproliferative activity against human HepG2 cells by MTT assay, IC50=8 μM
human DU145 cells Proliferation assay Antiproliferative activity against human DU145 cells by MTT assay, IC50=2 μM
mouse J774.A1 cells Proliferation assay 3 days Antiproliferative activity against mouse J774.A1 cells after 3 days by MTT conversion assay, IC50=0.003 μM
HEK293 cells Proliferation assay 3 days Antiproliferative activity against HEK293 cells after 3 days by MTT conversion assay, IC50=0.007 μM
mouse J774 cells Proliferation assay 72 h Antiproliferative activity against mouse J774 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.003 μM
human PBMC Function assay 4 days Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days, IC50=0.1495 μM
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells at lag phase of growth after 48 hrs by MTT assay, IC50=2.9 μM
A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells at lag phase of growth after 48 hrs by MTT assay, IC50=47 μM
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells at lag phase of growth after 48 hrs by MTT assay, IC50=1.4 μM
MT4 cells Cytotoxicity assay 96 h Cytotoxicity against human MT4 cells infected with HTLV-1 after 96 hrs by MTT assay, CC50=0.1 μM
CCRF-CEM cells Proliferation assay 96 h Antiproliferative activity against human CCRF-CEM cells after 96 hrs by MTT assay, CC50=1 μM
WIL2-NS cells Proliferation assay 96 h Antiproliferative activity against human WIL2-NS cells after 96 hrs by MTT assay, CC50=3 μM
CCRF-SB cells Proliferation assay 96 h Antiproliferative activity against human CCRF-SB cells after 96 hrs by MTT assay, CC50=1.1 μM
human DU145 cells Proliferation assay 96 h Antiproliferative activity against human DU145 cells after 96 hrs by MTT assay, CC50=2 μM
human HepG2 cells Proliferation assay 96 h Antiproliferative activity against human HepG2 cells after 96 hrs by MTT assay, CC50=8 μM
MCF7 cells Proliferation assay 96 h Antiproliferative activity against human MCF7 cells after 96 hrs by MTT assay, CC50=3.2 μM
SK-MEL-28 cells Proliferation assay 96 h Antiproliferative activity against human SK-MEL-28 cells after 96 hrs by MTT assay, CC50=15 μM
MCF7 cells Cytotoxicity assay Cytotoxicity against human MCF7 cells, IC50=2.79 μM
mouse S49 cells Cytotoxicity assay 72 h Cytotoxicity against wild type mouse S49 cells assessed as growth inhibition after 72 hrs by trypan blue exclusion assay, EC50=8 μM
Colo-357 cells Cytotoxicity assay Cytotoxicity against human Colo-357 cells by crystal violet staining, IC50=6.12 μM
Aspc-1 cells Cytotoxicity assay Cytotoxicity against human Aspc-1 cells by crystal violet staining, IC50=2.45 μM
A549 cells Cytotoxicity assay 48 h Cytotoxicity against human A549 cells assessed as cell viability after 48 hrs by MTT assay, IC50=47 μM
MCF7 cells Cytotoxicity assay 48 h Cytotoxicity against human MCF7 cells assessed as cell viability after 48 hrs by MTT assay, IC50=1.4 μM
Patu-02 cells Cytotoxicity assay Cytotoxicity against human Patu-02 cells by crystal violet staining, IC50=9.69 μM
Patu-T cells Cytotoxicity assay Cytotoxicity against human Patu-T cells by crystal violet staining, IC50=4.09 μM
Patu-S cells Cytotoxicity assay Cytotoxicity against human Patu-S cells by crystal violet staining, IC50=11.07 μM
T3M4 cells Cytotoxicity assay Cytotoxicity against human T3M4 cells by crystal violet staining, IC50=2.63 μM
human PANC1 cells Cytotoxicity assay Cytotoxicity against human PANC1 cells by crystal violet staining, IC50=6.39 μM
human DAN-G cells Cytotoxicity assay Cytotoxicity against human DAN-G cells by crystal violet staining, IC50=4.06 μM
HeLa cells Cytotoxicity assay 48 h Cytotoxicity against human HeLa cells assessed as cell viability after 48 hrs by MTT assay, IC50=2.9 μM
WEHI164 cells Proliferation assay 3 days Antiproliferative activity against mouse WEHI164 cells after 3 days by MTT conversion assay, IC50=0.015 μM
WIL-2NS cells Proliferation assay Antiproliferative activity against human WIL-2NS cells by MTT assay, IC50=3 μM
WEHI164 cells Proliferation assay 72 h Antiproliferative activity against mouse WEHI164 cells assessed as reduction of cell growth after 72 hrs by MTT method, IC50=0.017 μM
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Información química, almacenamiento y estabilidad (Chemical Information, Storage & Stability)

Peso molecular 152.18 Fórmula

C5H4N4S

Almacenamiento (Desde la fecha de recepción)
Nº CAS 50-44-2 Descargar SDF Almacenamiento de soluciones madre

Sinónimos 6-MP Smiles C1=NC2=C(N1)C(=S)N=CN2

Solubilidad (Solubility)

In vitro
Lote:

DMSO : 30 mg/mL (197.13 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:

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)

mg/kg g μL

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)

Targets/IC50/Ki
PRPP Amidotransferase
In vitro

Mercaptopurine (6-MP) is widely used to treat malignancies, rheumatic diseases, dermatologic conditions, inflammatory bowel disease, and solid organ transplant rejection. It inhibits purine nucleotide synthesis and metabolism by inhibiting an enzyme called Phosphoribosyl pyrophosphate amidotransferase (PRPP Amidotransferase). PRPP Amidotransferase is the rate limiting enzyme of purine synthesis. This compound alters the synthesis and function of RNA and DNA. It interferes with nucleotide interconversion and glycoprotein synthesis.

Referencias

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
NCT04770922 Completed
Acute Lymphoblastic Leukemia Pediatric|Adverse Drug Event
Cipherome Inc.|Stanford University
February 23 2021 --
NCT03022747 Unknown status
Lymphoblastic Leukemia Acute Childhood
Vastra Gotaland Region
January 2017 Phase 2