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Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibitor

Kat.-Nr.: S1305

Mercaptopurine (6-MP) ist ein weit verbreitetes Antileukämie-Mittel und Immunsuppressivum, das die De-novo-Purinsynthese durch die Inkorporation von Thiopurin-Methyltransferase-Metaboliten in DNA und RNA hemmt.
Mercaptopurine (6-MP) DNA/RNA Synthesis Inhibitor Chemical Structure

Chemische Struktur

Molekulargewicht: 152.18

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Qualitätskontrolle (Quality Control)

Charge: Reinheit: 99.97%
99.97

Zellkultur, Behandlung & Arbeitskonzentration
(Cell Culture, Treatment & Working Concentration)

Zelllinien Assay-Typ Konzentration Inkubationszeit Formulierung Aktivitätsbeschreibung 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
Klicken Sie hier, um weitere experimentelle Zellliniendaten anzuzeigen

Chemische Informationen, Lagerung & Stabilität (Chemical Information, Storage & Stability)

Molekulargewicht 152.18 Formel

C5H4N4S

Lagerung (Ab Erhaltdatum)
CAS-Nr. 50-44-2 SDF herunterladen Lagerung von Stammlösungen

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

Löslichkeit (Solubility)

In vitro
Charge:

DMSO : 30 mg/mL (197.13 mM)
(Feuchtigkeitskontaminiertes DMSO kann die Löslichkeit verringern. Verwenden Sie frisches, wasserfreies DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molaritätsrechner

Masse Konzentration Volumen Molekulargewicht
Verdünnungsrechner Molekulargewicht-Rechner

In vivo
Charge:

In-vivo-Formulierungsrechner (Klare Lösung)

Schritt 1: Geben Sie unten die Informationen ein (Empfohlen: Ein zusätzliches Tier einplanen, um Verluste während des Experiments auszugleichen)

mg/kg g μL

Schritt 2: Geben Sie die In-vivo-Formulierung ein (Dies ist nur der Rechner, nicht die Formulierung. Bitte kontaktieren Sie uns zuerst, wenn im Abschnitt Löslichkeit keine In-vivo-Formulierung angegeben ist.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

Berechnungsergebnisse:

Arbeitskonzentration: mg/ml;

Methode zur Herstellung der DMSO-Stammflüssigkeit: mg Wirkstoff voraufgelöst in μL DMSO ( Konzentration der Stammflüssigkeit mg/mL, Bitte kontaktieren Sie uns zuerst, wenn die Konzentration die DMSO-Löslichkeit der jeweiligen Wirkstoffcharge überschreitet. )

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzuμL PEG300, mischen und aufklären, fügen Sie als Nächstes hinzuμL Tween 80, mischen und aufklären, fügen Sie als Nächstes hinzu μL ddH2O, mischen und aufklären.

Methode zur Herstellung der In-vivo-Formulierung: Nehmen Sie μL DMSO Stammflüssigkeit, fügen Sie als Nächstes hinzu μL Maisöl, mischen und aufklären.

Hinweis: 1. Bitte stellen Sie sicher, dass die Flüssigkeit klar ist, bevor Sie das nächste Lösungsmittel hinzufügen.
2. Achten Sie darauf, die Lösungsmittel in der richtigen Reihenfolge hinzuzufügen. Sie müssen sicherstellen, dass die im vorherigen Schritt erhaltene Lösung klar ist, bevor Sie das nächste Lösungsmittel hinzufügen. Physikalische Methoden wie Vortexen, Ultraschall oder ein warmes Wasserbad können zur Unterstützung des Lösungsvorgangs verwendet werden.

Wirkungsmechanismus (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.

Referenzen

Informationen zu klinischen Studien (Clinical Trial Information)

(Daten von https://clinicaltrials.gov, aktualisiert am 2026-07-30)

NCT-Nummer Rekrutierung Bedingungen Sponsor/Kollaboratoren Startdatum Phases
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