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

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Controllo Qualità (Quality Control)

Lotto: Purezza: 99.97%

99.97

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

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Linee cellulari	Tipo di saggio	Tempo di incubazione	Descrizione dell'attività
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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Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Peso molecolare	152.18	Formula	C₅H₄N₄S	Conservazione (Dalla data di ricezione)	3 anni-20°Cpolvere
N. CAS	50-44-2	Scarica SDF		Conservazione delle soluzioni stock	1 anno-80°Cin solvente 1 mese-20°Cin solvente
Sinonimi	6-MP			Smiles	C1=NC2=C(N1)C(=S)N=CN2

Solubilità (Solubility)

In vitro
Lotto:

DMSO : 30 mg/mL (197.13 mM)
(Il DMSO contaminato da umidità può ridurre la solubilità. Utilizzare DMSO fresco e anidro.)

Water : Insoluble

Ethanol : Insoluble

Calcolatore di Molarità

Massa	Concentrazione	Volume	Peso molecolare
=	×	×

Calcolatore di Diluizione Calcolatore del Peso Molecolare

In vivo Lotto:
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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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 Validato dai laboratori Selleck. Se necessiti di modifiche a questa formulazione, contatta il nostro team di vendita per test personalizzati.	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.

Calcolatore di formulazione in vivo (Soluzione chiara)

Passo 1: Inserire le informazioni di seguito (Consigliato: Un animale aggiuntivo per tenere conto della perdita durante l'esperimento)

Dosaggio: mg/kg Peso medio degli animali: g Volume di dosaggio per animale:μL Numero di animali:

Passo 2: Inserire la formulazione in vivo (Questo è solo il calcolatore, non la formulazione. Contattateci prima se non c'è una formulazione in vivo nella sezione Solubilità.)

% DMSO + % + % Tween 80 + % ddH₂O

%DMSO+ %

Risultati del calcolo:

Concentrazione di lavoro: mg/ml;

Metodo per preparare il liquido master di DMSO: mg farmaco predissolto in μL DMSO ( Concentrazione del liquido master mg/mL, Vi preghiamo di contattarci prima se la concentrazione supera la solubilità del DMSO del lotto del farmaco. )

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungereμL PEG300, mescolare e chiarire, quindi aggiungereμL Tween 80, mescolare e chiarire, quindi aggiungere μL ddH₂O, mescolare e chiarire.

Metodo per preparare la formulazione in vivo: Prendere μL DMSO liquido master, quindi aggiungere μL Olio di mais, mescolare e chiarire.

Nota: 1. Si prega di assicurarsi che il liquido sia limpido prima di aggiungere il solvente successivo.
2. Assicurarsi di aggiungere il/i solvente/i in ordine. È necessario assicurarsi che la soluzione ottenuta, nell'aggiunta precedente, sia una soluzione limpida prima di procedere all'aggiunta del solvente successivo. Metodi fisici come il vortex, gli ultrasuoni o il bagno d'acqua calda possono essere utilizzati per facilitare la dissoluzione.

Meccanismo d'azione (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.
Riferimenti	[1] https://pubmed.ncbi.nlm.nih.gov/18506437/ [2] https://pubmed.ncbi.nlm.nih.gov/7191632/

Informazioni sullo studio clinico (Clinical Trial Information)

(dati da https://clinicaltrials.gov, aggiornato il 2024-05-22)

Numero NCT	Reclutamento	Condizioni	Sponsor/Collaboratori	Data di inizio	Fasi
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

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

Mercaptopurine (6-MP) DNA/RNA Synthesis Inibitore

Peso molecolare: 152.18

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Informazioni sullo studio clinico (Clinical Trial Information)

Mercaptopurine (6-MP) DNA/RNA Synthesis Inibitore

Peso molecolare: 152.18

Controllo Qualità (Quality Control)

Coltura cellulare, trattamento e concentrazione di lavoro (Cell Culture, Treatment & Working Concentration)

Informazioni chimiche, conservazione e stabilità (Chemical Information, Storage & Stability)

Solubilità (Solubility)

Calcolatore di Molarità

Calcolatore di formulazione in vivo (Soluzione chiara)

Meccanismo d'azione (Mechanism of Action)

Informazioni sullo studio clinico (Clinical Trial Information)

Coltura cellulare, trattamento e concentrazione di lavoro
(Cell Culture, Treatment & Working Concentration)