Name: Mercaptopurine (6-MP)
Brand: Selleck Chemicals
SKU: S1305
Rating: 5 (16 reviews)

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Kwaliteitscontrole (Quality Control)

Batch: Zuiverheid: 99.97%

99.97

Gerelateerde doelwitten	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
Overig DNA/RNA Synthesis Inhibitoren	CX-5461 (Pidnarulex) SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Carmofur Triapine (3-AP) YK-4-279 Halofuginone

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

Cellijnen	Assaytype	Incubatietijd	Activiteitsbeschrijving
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)	3 jaar-20°Cpoeder
CAS-nr.	50-44-2	SDF downloaden		Opslag van stamoplossingen	1 jaar-80°Cin oplosmiddel 1 maand-20°Cin oplosmiddel
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:
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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	1.250mg/ml (8.21mM)	Taking the 1 mL working solution as an example, add 50 μL of 25 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 Gevalideerd door Selleck labs. Mocht u aanpassingen aan deze formulering nodig hebben, neem dan contact op met ons verkoopteam voor aangepaste tests.	0.208mg/ml (1.37mM)	Taking the 1 mL working solution as an example, add 50 μL of 4.16 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.

In vivo formulatiecalculator (heldere oplossing)

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

Dosering: mg/kg Gemiddeld gewicht van dieren: g Doseervolume per dier:μL Aantal dieren:

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) wordt veel gebruikt voor de behandeling van maligniteiten, reumatische aandoeningen, dermatologische aandoeningen, inflammatoire darmziekten en afstoting van vaste orgaantransplantaten. Het remt de synthese en het metabolisme van purine-nucleotiden door een enzym genaamd Phosphoribosylpyrophosphaat-amidotransferase (PRPP-amidotransferase) te remmen. PRPP-amidotransferase is het snelheidsbepalende enzym van de purinesynthese. Deze verbinding verandert de synthese en functie van RNA en DNA. Het interfereert met de interconversie van nucleotiden en de synthese van glycoproteïnen.
Referenties	[1] https://pubmed.ncbi.nlm.nih.gov/18506437/ [2] https://pubmed.ncbi.nlm.nih.gov/7191632/

Informatie over klinische proeven (Clinical Trial Information)

(gegevens van https://clinicaltrials.gov, bijgewerkt op 2024-05-22)

NCT-nummer	Werving	Aandoeningen	Sponsor/medewerkers	Startdatum	Fasen
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

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Mercaptopurine (6-MP) DNA/RNA Synthesis inhibitor

Chemische structuur

Molecuulgewicht: 152.18

Kwaliteitscontrole (Quality Control)

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

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

Mercaptopurine (6-MP) DNA/RNA Synthesis inhibitor

Chemische structuur

Molecuulgewicht: 152.18

Kwaliteitscontrole (Quality Control)

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

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

Oplosbaarheid (Solubility)

Molariteitscalculator

In vivo formulatiecalculator (heldere oplossing)

Werkingsmechanisme (Mechanism of Action)

Informatie over klinische proeven (Clinical Trial Information)

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