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Mercaptopurine (6-MP) DNA/RNA Synthesis Remmer

Cat.nr.: S1305

Mercaptopurine (6-MP) is een veelgebruikt antileukemisch middel en immuunsuppressief medicijn dat de de-novo-purinesynthese remt door incorporatie van thiopurine-methyltransferase-metabolieten in DNA en RNA.
Mercaptopurine (6-MP) DNA/RNA Synthesis Remmer Chemical Structure

Chemische structuur

Molecuulgewicht: 152.18

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.97%
99.97

Celkweek, behandeling & werkzame concentratie
(Cell Culture, Treatment & Working Concentration)

Cellijnen Assaytype Concentratie Incubatietijd Formulering Activiteitsbeschrijving 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
Klik om meer experimentele gegevens over cellijnen te bekijken

Chemische informatie, opslag en stabiliteit (Chemical Information, Storage & Stability)

Molecuulgewicht 152.18 Formule

C5H4N4S

Opslag (vanaf de datum van ontvangst)
CAS-nr. 50-44-2 SDF downloaden Opslag van stamoplossingen

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

Oplosbaarheid (Solubility)

In vitro
Batch:

DMSO : 30 mg/mL (197.13 mM)
(Met vocht verontreinigd DMSO kan de oplosbaarheid verminderen. Gebruik verse, watervrije DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molariteitscalculator

Massa Concentratie Volume Molecuulgewicht
Verdunningscalculator Molecuulgewichtcalculator

In vivo
Batch:

In vivo formulatiecalculator (heldere oplossing)

Stap 1: Voer onderstaande informatie in (Aanbevolen: een extra dier om rekening te houden met verlies tijdens het experiment)

mg/kg g μL

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 de sectie oplosbaarheid.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berekeningsresultaten:

Werkconcentratie: mg/ml;

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

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toeμL PEG300, mengen en verhelderen, daarna toevoegenμL Tween 80, mengen en verhelderen, daarna toevoegen μL ddH2O, mengen en verhelderen.

Methode voor het bereiden van in vivo formulering: Neem μL DMSO moedervloeistof, voeg daarna toe μL Maïsolie, mengen en verhelderen.

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. Fysieke methoden zoals vortexen, ultrasoon of een warmwaterbad kunnen worden gebruikt om het oplossen te bevorderen.

Werkingsmechanisme (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.

Referenties

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2026-07-30)

NCT-nummer Werving Aandoeningen Sponsor/medewerkers Startdatum Fasen
NCT07072585 NOT_YET_RECRUITING
Stage II T Lymphoblastic Leukemia/Lymphoma; Stage III T Lymphoblastic Leukemia/Lymphoma; Stage IV T Lymphoblastic Leukemia/Lymphoma; T Acute Lymphoblastic Leukemia; T Lymphoblastic Lymphoma
Children's Oncology Group
2026-08-28 PHASE2; PHASE3
NCT07716735 NOT_YET_RECRUITING
Advanced Kidney Carcinoma; Advanced Renal Cell Carcinoma; Hereditary Leiomyomatosis and Renal Cell Carcinoma; Metastatic Kidney Carcinoma; Metastatic Renal Cell Carcinoma; Skin Leiomyoma; Stage III Renal Cell Cancer AJCC v8; Stage IV Renal Cell Cancer AJCC v8; Uterine Corpus Leiomyoma
Jonsson Comprehensive Cancer Center
2026-12-01 PHASE1
NCT06099366 RECRUITING
Lymphoblastic Leukemia in Children
Hee Young Ju
2024-03-05 PHASE2
NCT03959085 RECRUITING
B Acute Lymphoblastic Leukemia; B Lymphoblastic Lymphoma; Central Nervous System Leukemia; Mixed Phenotype Acute Leukemia; Testicular Leukemia
Children's Oncology Group
2019-10-31 PHASE3
NCT07636564 NOT_YET_RECRUITING
Acute Leukemia of Ambiguous Lineage; B Acute Lymphoblastic Leukemia; B Acute Lymphoblastic Leukemia, Philadelphia Chromosome Negative; T Acute Lymphoblastic Leukemia
SWOG Cancer Research Network
2026-10-14 PHASE2
NCT07431060 RECRUITING
Langerhans Cell Histiocytosis (LCH)
West China Second University Hospital
2026-02-13