Name: Mercaptopurine (6-MP)
Brand: Selleck Chemicals
SKU: S1305
Availability: InStock
Rating: 5 (15 reviews)

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Quality Control

Batch: Purity: 99.97%

99.97

Related Targets	HDAC PARP ATM/ATR DNA-PK WRN Topoisomerase PPAR Sirtuin Casein Kinase eIF
Other DNA/RNA Synthesis Inhibitors	CX-5461 (Pidnarulex) B02 SCR7 Favipiravir (T-705) EED226 RK-33 BMH-21 Triapine (3-AP) Carmofur YK-4-279

Cell Culture, Treatment & Working Concentration

Cell Lines	Assay Type	Incubation Time	Activity Description
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
Click to View More Cell Line Experimental Data

Solubility

In vitro
Batch:

DMSO : 30 mg/mL (197.13 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : Insoluble

Ethanol : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection 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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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 Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	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 Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)

% DMSO

%

% Tween 80

% ddH₂O

% DMSO

+

%

Calculation results:

Working concentration: mg/ml;

Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH₂O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such
as vortex, ultrasound or hot water bath can be used to aid dissolving.

Chemical Information, Storage & Stability

Molecular Weight	152.18	Formula	C₅H₄N₄S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	50-44-2	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	6-MP			Smiles	C1=NC2=C(N1)C(=S)N=CN2

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.
References	[1] https://pubmed.ncbi.nlm.nih.gov/18506437/ [2] https://pubmed.ncbi.nlm.nih.gov/7191632/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	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

Tech Support

Handling Instructions

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Mercaptopurine (6-MP) DNA/RNA Synthesis inhibitor

Chemical Structure

Molecular Weight: 152.18