Azathioprine
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.
For research use only. We do not sell to patients.
- Purity: 99.99%
- CAS No.: 446-86-6
- Formula: C9H7N7O2S
- Molecular Weight:277.26
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) Azathioprine
More- ACS Environ Au. 2025 Aug 5;5(6):573-582. [Abstract]
- Anal Chem. 2025 Jun 3;97(21):11099-11109. [Abstract]
- Cell Rep Methods. 2023 Oct 23;3(10):100599. [Abstract]
- APL Bioeng. 2023 Aug 11;7(3):036108. [Abstract]
- Comput Struct Biotechnol J. 2023 Feb 24:21:1907-1920. [Abstract]
- Biotechnol Bioeng. 2021 Dec;118(12):4687-4698. [Abstract]
- PLoS Negl Trop Dis. 2019 Aug 20;13(8):e0007681. [Abstract]
- European University of Valencia. 2025.
Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| B cell | IC50 |
1 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in human B cell assessed as inhibition of mitogenesis
Immunosuppressive activity in human B cell assessed as inhibition of mitogenesis
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[PMID: 3373220] |
| B-cell | IC50 |
2.7 μg/mL
Compound: azathioprine
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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
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[PMID: 14738397] |
| Lymphocyte | IC50 |
2.9 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay
Immunosuppressive activity in baboon lymphocytes by mixed lymphocyte reaction assay
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[PMID: 3373220] |
| Lymphocyte | IC50 |
3 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
Immunosuppressive activity in human lymphocytes by mixed lymphocyte reaction assay
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[PMID: 3373220] |
| Lymphocyte | IC50 |
85 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in human lymphocytes assessed as inhibition of protein synthesis
Immunosuppressive activity in human lymphocytes assessed as inhibition of protein synthesis
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[PMID: 3373220] |
| PBMC | IC50 |
230.4 nM
Compound: azathioprine
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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
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[PMID: 18467007] |
| Sf21 | IC50 |
>1000 μM
Compound: Azathioprine
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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
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[PMID: 21965623] |
| Sf21 | IC50 |
>1000 μM
Compound: Azathioprine
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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
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[PMID: 21965623] |
| T-cell | IC50 |
0.4 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in baboon T cell assessed as inhibition of mitogenesis
Immunosuppressive activity in baboon T cell assessed as inhibition of mitogenesis
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[PMID: 3373220] |
| T-cell | IC50 |
2 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in rat T cell assessed as inhibition of mitogenesis
Immunosuppressive activity in rat T cell assessed as inhibition of mitogenesis
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[PMID: 3373220] |
| T-cell | IC50 |
2.7 μg/mL
Compound: azathioprine
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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
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[PMID: 14738397] |
| T-cell | IC50 |
2.7 μg/mL
Compound: Azathioprine
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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
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[PMID: 11575965] |
| T-cell | IC50 |
9 μg/mL
Compound: Azathioprine
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Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis
Immunosuppressive activity in human T cell assessed as inhibition of mitogenesis
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[PMID: 3373220] |
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.
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Cell Line:Rat hepatocytes, Human hepatocytes
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Concentration:0-50 μM
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Incubation Time:24-48 hours
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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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Outbred female CD-1 mice, Female ICR mice[3]
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Dosage:25-400 mg/kg
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Administration:Oral gavage; everyday; 10days
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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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 446-86-6
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Appearance Solid
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Molecular Weight 277.26
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Formula C9H7N7O2S
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Color Light yellow to yellow
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SMILES
O=[N+](C1=C(SC2=C3NC=NC3=NC=N2)N(C)C=N1)[O-]
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Synonyms
BW 57-322
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Publications (8)
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Journal Impact Factor
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Most Recent
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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 -
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (283 KB)
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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)
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Handling Instructions (2659 KB)
References
[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]
Complete Stock Solution Preparation Table
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.
| 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 |
Azathioprine Related Classifications
HY-B0256 Related Classifications
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