Art. -Nr.: HY-B0256

Azathioprine

(Synonyms: BW 57-322)

8 Cited Publications

Kundenbewertung

Based on 8 publication(s) in Google Scholar

Azathioprine (BW 57-322) is an orally active immunosuppressive agent. Azathioprine can be converted in vivo to the active metabolite 6-mercaptopurine (6-MP). Azathioprine has myelosuppressive effects and induces apoptosis.

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Reinheit: 99.99%
CAS. Nr.: 446-86-6
Formel: C₉H₇N₇O₂S
Molecular Weight:277.26

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Azathioprine Chemical Structure

CAS. Nr.: 446-86-6

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Publications (8)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
B cell	IC₅₀	1 μg/mL Compound: Azathioprine	Immunosuppressive activity in human B cell assessed as inhibition of mitogenesis Immunosuppressive activity in human B cell assessed as inhibition of mitogenesis	[PMID: 3373220]
B-cell	IC₅₀	2.7 μg/mL Compound: azathioprine	Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic B lymphocytes assessed as inhibition of LPS-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
Lymphocyte	IC₅₀	2.9 μg/mL Compound: Azathioprine	Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
Lymphocyte	IC₅₀	3 μg/mL Compound: Azathioprine	Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay	[PMID: 3373220]
Lymphocyte	IC₅₀	85 μg/mL Compound: Azathioprine	Immunosuppressive activity in human lymphocytes assessed as inhibition of protein synthesis Immunosuppressive activity in human lymphocytes assessed as inhibition of protein synthesis	[PMID: 3373220]
PBMC	IC₅₀	230.4 nM Compound: azathioprine	Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days Inhibition of T cell mitogen-induced blastogenesis in human PBMC after 4 days	[PMID: 18467007]
Sf21	IC₅₀	>1000 μM Compound: Azathioprine	Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of human BSEP expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
Sf21	IC₅₀	>1000 μM Compound: Azathioprine	Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake Inhibition of Sprague-Dawley rat Bsep expressed in plasma membrane vesicles of Sf21 cells assessed as inhibition of ATP-dependent [3H]taurocholate uptake	[PMID: 21965623]
T-cell	IC₅₀	0.4 μg/mL Compound: Azathioprine	Immunosuppressive activity in baboon T cell assessed as inhibition of mitogenesis Immunosuppressive activity in baboon T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	2 μg/mL Compound: Azathioprine	Immunosuppressive activity in rat T cell assessed as inhibition of mitogenesis Immunosuppressive activity in rat T cell assessed as inhibition of mitogenesis	[PMID: 3373220]
T-cell	IC₅₀	2.7 μg/mL Compound: azathioprine	Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay Immunosuppressive activity in BALB/c mouse splenic T lymphocytes assessed as inhibition of Con A-induced cell proliferation after 72 hrs by MTT assay	[PMID: 14738397]
T-cell	IC₅₀	2.7 μg/mL Compound: Azathioprine	Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation Immunosuppressant activity in mouse T cells assessed as inhibition of concanavalin A-induced cell proliferation	[PMID: 11575965]
T-cell	IC₅₀	9 μg/mL Compound: Azathioprine	Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis	[PMID: 3373220]

In Vitro

Azathioprine (0-50 μM, 48 hours) can induce severe intracellular GSH depletion with relevant concentrations in both primary rat and human hepatocytes^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay^[2]

Cell Line:

Rat hepatocytes, Human hepatocytes
Concentration:

0-50 μM
Incubation Time:

24-48 hours
Result:

Showed the decrease in cell viability and intracellular GSH levels in rat hepatocytes as low concentration of 0.5 μM but no significant decrease in cell viability at concentrations below 50 μM as well as GSH depletion was obviously noted at a concentration as low as 1 μM in human hepatocytes.

In Vivo

Azathioprine (oral gavage, 25-400 mg/kg, everyday, 10days) can affect bone marrow cells, red blood cells, and peripheral blood cytokines and other related parameters in a dose-dependent manner, and can induce apoptosis in female CD-1 mice and ICR mice^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Outbred female CD-1 mice, Female ICR mice^[3]
Dosage:

25-400 mg/kg
Administration:

Oral gavage; everyday; 10days
Result:

Induced a decrease in erythrocyte-related parameters as well as leukocyte-related parameters in a dose-dependent manner.
Induced 52.4%, 35.4%, 17.9%, 16.1% and 15.2% reduction in bone marrow cells at concentrations of 40, 60, 80, 100 and 120 mg/kg, respectively while fms-like tyrosine kinase-3(FLT-3) ligand (FL)-related cytokines were increased.

Clinical Trial

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS. Nr. 446-86-6
Appearance Solid
Molecular Weight 277.26
Formel C₉H₇N₇O₂S
Color Light yellow to yellow
SMILES

O=[N+](C1=C(SC2=C3NC=NC3=NC=N2)N(C)C=N1)[O-]
Synonyms

BW 57-322
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Publications (8)

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ACS Environ Au

Machine Learning-Assisted Recognition of Environmental Sulfur-Containing Chemicals in Nontargeted Mass Spectrometry Analysis of Inadequate Mass Resolution. [Abstract]

2025 Aug 5;5(6):573-582. PMID: 41277996
Anal Chem

Exposome-Scale Investigation of Cl-/Br-Containing Chemicals Using High-Resolution Mass Spectrometry, Multistage Machine Learning, and Cloud Computing. [Abstract]

2025 Jun 3;97(21):11099-11109. PMID: 40401576
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
APL Bioeng

Fluid shear stress enhances natural killer cell's cytotoxicity toward circulating tumor cells through NKG2D-mediated mechanosensing. [Abstract]

2023 Aug 11;7(3):036108. PMID: 37575881
Comput Struct Biotechnol J

Network Proximity-based computational pipeline identifies drug candidates for different pathological stages of Alzheimer's disease. [Abstract]

2023 Feb 24:21:1907-1920. PMID: 36936813
Biotechnol Bioeng

An integrated biomimetic array chip for establishment of collagen-based 3D primary human hepatocyte model for prediction of clinical drug-induced liver injury. [Abstract]

2021 Dec;118(12):4687-4698. PMID: 34478150
PLoS Negl Trop Dis

Identification of anti-flaviviral drugs with mosquitocidal and anti-Zika virus activity in Aedes aegypti. [Abstract]

2019 Aug 20;13(8):e0007681. PMID: 31430351
European University of Valencia

2025.

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (180.34 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

H₂O : < 0.1 mg/mL (insoluble)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

3.6067 mL

18.0336 mL

36.0672 mL

5 mM

0.7213 mL

3.6067 mL

7.2134 mL

10 mM

0.3607 mL

1.8034 mL

3.6067 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.08 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.08 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.08 mg/mL (7.50 mM); Clear solution

This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (283 KB)
SDS (558 KB)
- English - EN (558 KB)
- Français - FR (558 KB)
- Deutsch - DE (558 KB)
- Norwegian - NO (558 KB)
- Español - ES (558 KB)
- Swedish - SV (558 KB)
- Italian - IT (558 KB)
- Korean - KR (558 KB)
- Portuguese - PT (558 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Patel, A.A., R.A. Swerlick, and C.O. McCall, Azathioprine in dermatology: the past, the present, and the future. J Am Acad Dermatol, 2006. 55(3): p. 369-89. [Content Brief]

[2]. Maltzman, J.S. and G.A. Koretzky, Azathioprine: old drug, new actions. J Clin Invest, 2003. 111(8): p. 1122-4. [Content Brief]

[3]. Dubinsky, M.C., Azathioprine, 6-mercaptopurine in inflammatory bowel disease: pharmacology, efficacy, and safety. Clin Gastroenterol Hepatol, 2004. 2(9): p. 731-43. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.6067 mL	18.0336 mL	36.0672 mL	90.1681 mL
	5 mM	0.7213 mL	3.6067 mL	7.2134 mL	18.0336 mL
	10 mM	0.3607 mL	1.8034 mL	3.6067 mL	9.0168 mL
	15 mM	0.2404 mL	1.2022 mL	2.4045 mL	6.0112 mL
	20 mM	0.1803 mL	0.9017 mL	1.8034 mL	4.5084 mL
	25 mM	0.1443 mL	0.7213 mL	1.4427 mL	3.6067 mL
	30 mM	0.1202 mL	0.6011 mL	1.2022 mL	3.0056 mL
	40 mM	0.0902 mL	0.4508 mL	0.9017 mL	2.2542 mL
	50 mM	0.0721 mL	0.3607 mL	0.7213 mL	1.8034 mL
	60 mM	0.0601 mL	0.3006 mL	0.6011 mL	1.5028 mL
	80 mM	0.0451 mL	0.2254 mL	0.4508 mL	1.1271 mL
	100 mM	0.0361 mL	0.1803 mL	0.3607 mL	0.9017 mL

Keywords

Azathioprine

8 Cited Publications

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Azathioprine

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Publications Citing Use of MedChemExpress (MCE) Azathioprine

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Azathioprine

Apoptosis Compound Library

Immunology/Inflammation Compound Library

FDA-Approved Drug Library

Anti-Cancer Compound Library

Drug Repurposing Compound Library

Nucleotide Compound Library

NMPA-Approved Drug Library

Orally Active Compound Library

FDA Approved & Pharmacopeial Drug Library

Drug-Induced Liver Injury (DILI) Compound Library

Tumorigenesis-Related Compound Library

Rare Diseases Drug Library

FDA-Approved Anticancer Drug Library

Human Metabolite Library

Anti-Pulmonary Fibrosis Compound Library

Non-steroidal Anti-Inflammatory Compound Library

Heterocyclic Compound Library

Off-patent Drug Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

FDA-Approved Drug Library Plus

FDA-Approved Drug Library Mini

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

Publications Citing Use of MedChemExpress (MCE) Azathioprine

Biologische Aktivität

Chemical Information

Publications (8)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Azathioprine Related Classifications

HY-B0256 Related Classifications