Catalog No.S1721

For research use only.

Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

Azathioprine Chemical Structure

CAS No. 446-86-6

Selleck's Azathioprine has been cited by 2 Publications

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Biological Activity

Description Azathioprine is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.
Rac1 [1]
In vitro

Azathioprine suppresses the activation of Rac1 target genes such as mitogen-activated protein kinase kinase (MEK), NF-kappaB, and bcl-x(L), leading to a mitochondrial pathway of apoptosis in primary human CD4+ T lymphocytes. Azathioprine thus converts a costimulatory signal into an apoptotic signal by modulating Rac1 activity. [1] Azathioprine-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. [2] Azathioprine (1 mM) restores ATP levels and arrests cell injury, while culture in glucose-enriched media augments ATP levels and ameliorates cell death. Azathioprine reduces viability 5-34% at day 1 and 42-92% by day 4. [3] Azathioprine decreases the viability of hepatocytes and induces the following events in primary culture of isolated rat hepatocytes: intracellular reduces glutathione (GSH) depletion, metabolic activity reduction, and lactate dehydrogenase release. Azathioprine effect on hepatocytes is associated with swelling and increased oxygen consumption of intact isolated rat liver mitochondria. [4]

In vivo Azathioprine combined with cyclosporin A and prednisolone has resulted in survival of 14 out of 15 grafts (93%), compared with 11 out of 14 (79%) in the group treated with cyclosporin A alone in mouse-rat brain xenograft. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

DMSO 54 mg/mL
(194.76 mM)
Water Insoluble
Ethanol Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 277.26


CAS No. 446-86-6
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-]

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

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT04109300 Not yet recruiting Genetic: HLADQA1*05A>G screening|Other: Standard of Care Inflammatory Bowel Diseases|Ulcerative Colitis|Crohn Disease Western University Canada September 1 2020 Not Applicable
NCT03350633 Completed Drug: Tocilizumab Injection|Drug: Azathioprine Neuromyelitis Optica Spectrum Disorders|Neuromyelitis Optica Tianjin Medical University General Hospital November 1 2017 Phase 2|Phase 3
NCT02598596 Completed Biological: Pegloticase|Drug: Azathioprine Gout Ampel BioSolutions LLC|IND 2 Results LLC December 2015 Phase 2
NCT01160276 Completed Drug: cyclosporine+colchicine|Drug: tacrolimus Renal Replacement Therapies Assistance Publique - Hôpitaux de Paris|Institut National de la Santé Et de la Recherche Médicale France May 2010 Phase 1

(data from, updated on 2022-01-17)

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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