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Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibiteur

Réf. Catalogue: S1305

Mercaptopurine (6-MP) est un agent antileucémique et un médicament immunosuppresseur largement utilisé qui inhibe la synthèse de novo des purines par l'incorporation de métabolites de la thiopurine méthyltransférase dans l'ADN et l'ARN.
Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibiteur Chemical Structure

Structure chimique

Poids moléculaire: 152.18

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Contrôle Qualité (Quality Control)

Lot : Pureté : 99.97%
99.97

Culture cellulaire, traitement et concentration de travail
(Cell Culture, Treatment & Working Concentration)

Lignées cellulaires Type d'essai Concentration Temps d'incubation Formulation Description de l'activité 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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Informations chimiques, stockage et stabilité (Chemical Information, Storage & Stability)

Poids moléculaire 152.18 Formule

C5H4N4S

Stockage (À compter de la date de réception)
N° CAS 50-44-2 Télécharger le SDF Stockage des solutions mères

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

Solubilité (Solubility)

In vitro
Lot:

DMSO : 30 mg/mL (197.13 mM)
(Le DMSO contaminé par l'humidité peut réduire la solubilité. Utiliser du DMSO frais et anhydre.)

Water : Insoluble

Ethanol : Insoluble

Calculateur de molarité

Masse Concentration Volume Poids moléculaire
Calculateur de dilution Calculateur de poids moléculaire

In vivo
Lot:

Calculateur de formulation in vivo (Solution claire)

Étape 1 : Saisir les informations ci-dessous (Recommandé : Un animal supplémentaire pour tenir compte des pertes pendant l'expérience)

mg/kg g μL

Étape 2 : Saisir la formulation in vivo (Ceci est seulement le calculateur, pas la formulation. Veuillez nous contacter d'abord s'il n'y a pas de formulation in vivo dans la section Solubilité.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Résultats du calcul :

Concentration de travail : mg/ml;

Méthode de préparation du liquide maître DMSO : mg médicament prédissous dans μL DMSO ( Concentration du liquide maître mg/mL, Veuillez nous contacter d'abord si la concentration dépasse la solubilité du DMSO du lot de médicament. )

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouterμL PEG300, mélanger et clarifier, puis ajouterμL Tween 80, mélanger et clarifier, puis ajouter μL ddH2O, mélanger et clarifier.

Méthode de préparation de la formulation in vivo : Prendre μL DMSO liquide maître, puis ajouter μL Huile de maïs, mélanger et clarifier.

Note : 1. Veuillez vous assurer que le liquide est clair avant d'ajouter le solvant suivant.
2. Assurez-vous d'ajouter le(s) solvant(s) dans l'ordre. Vous devez vous assurer que la solution obtenue, lors de l'ajout précédent, est une solution claire avant de procéder à l'ajout du solvant suivant. Des méthodes physiques telles que le vortex, les ultrasons ou le bain-marie chaud peuvent être utilisées pour faciliter la dissolution.

Mécanisme d'action (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.

Références

Informations sur l'essai clinique (Clinical Trial Information)

(données du https://clinicaltrials.gov, mis à jour le 2024-05-22)

Numéro NCT Recrutement Conditions Promoteur/Collaborateurs Date de début Phases
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