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Azathioprine Rho inhibitor

Name: Azathioprine
Brand: Selleck Chemicals
SKU: S1721
Availability: InStock
Rating: 5 (7 reviews)

Cat.No.S1721

Azathioprine(BW 57-322) is an immunosuppressive drug, inhibiting purine synthesis and GTP-binding protein Rac1 activation, used in the treatment of organ transplantation and autoimmune diseases.

Chemical Structure

Molecular Weight: 277.26

Jump to Mechanism of Action Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.99%

99.99

Related Targets	DNA/RNA Synthesis CDK Microtubule Associated Ras HSP PD-1/PD-L1 Aurora Kinase Casein Kinase Serine/threonin kinase eIF Chk ROCK Myc Kinesin PLK DHFR PAK PERK DYRK RUNX PP2A PFKFB AP-1 MPS1 Wee1 p21 BMI-1 LIM kinase Nur77 APC
Related Products	NSC 23766 trihydrochloride CCG-1423 EHop-016 ML141 EHT 1864 2HCl ZCL278 MBQ-167 CCG-203971 Rhosin hydrochloride CID44216842 RhoGDI Antibody [H2N24] CASIN CDC42 Antibody [B4N7] TC10 Antibody [D5M19] CCG-100602 SRF Antibody [N16D21] CCG-222740 Rho A Antibody [G4B13] RP-102124 Rho Antibody [B24D19] Rac1 Antibody [D22N1] MLS-573151 RhoE Antibody [A21D22] Phospho-VAV1 (Tyr174) Antibody [K4A21] 1A-116 SAR407899 hydrochloride Rac1 + Rac2 + Rac3 Antibody [G9P16] MLS000532223 VAV2 Antibody [B11L17] RhoA Antibody [B21G13]

Chemical Information, Storage & Stability

Molecular Weight	277.26	Formula	C₉H₇N₇O₂S	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	446-86-6	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	BW 57-322			Smiles	CN1C=NC(=C1SC2=NC=NC3=C2NC=N3)[N+](=O)[O-]

Solubility

In vitro
Batch:

DMSO : 54 mg/mL (194.76 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.
Clear solution	5% DMSO 1 50%PEG300 2 5%Tween80 3 40%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	1.000mg/ml (3.61mM)	Taking the 1 mL working solution as an example, add 50 μL of 20 mg/ml clarified DMSO stock solution to 500 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 400 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.

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.

Mechanism of Action

Targets/IC₅₀/Ki	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. This compound thus converts a costimulatory signal into an apoptotic signal by modulating Rac1 activity. ^[1] This compound-generated 6-Thio-GTP thus prevents the development of an effective immune response via blockade of Vav activity on Rac proteins. ^[2] This chemical (1 mM) restores ATP levels and arrests cell injury, while culture in glucose-enriched media augments ATP levels and ameliorates cell death. It reduces viability 5-34% at day 1 and 42-92% by day 4. ^[3] This agent 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. Its 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]
References	[1] https://pubmed.ncbi.nlm.nih.gov/12697733/ [2] https://pubmed.ncbi.nlm.nih.gov/16365460/ [3] https://pubmed.ncbi.nlm.nih.gov/15123360/ [4] https://pubmed.ncbi.nlm.nih.gov/15226385/ [5] https://pubmed.ncbi.nlm.nih.gov/8566182/

Clinical Trial Information

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

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
NCT06066957	Recruiting	Cytomegalovirus Infections\|Transplant-Related Disorder	University of Pennsylvania\|Merck Sharp & Dohme LLC	April 4 2024	Phase 2
NCT05859191	Recruiting	Systemic Lupus Erythematosus\|Physiopathology	University Hospital Tours\|Research Center for Respiratory Diseases Inserm U1100	July 21 2023	--
NCT05994716	Enrolling by invitation	Inflammatory Bowel Diseases\|Crohn Disease\|Ulcerative Colitis	Research and Practical Clinical Center for Diagnostics and Telemedicine Technologies of the Moscow Health Care Department\|Sechenov University	April 25 2023	Not Applicable
NCT05349006	Not yet recruiting	Central Nervous System Inflammation\|MOG-IgG Associated Disease	Hospices Civils de Lyon	January 1 2023	Phase 3
NCT05370690	Unknown status	Uveitis	University Hospital Brest	May 1 2022	--
NCT05321485	Unknown status	Inflammatory Bowel Diseases\|Crohn Disease\|Ulcerative Colitis	Maxima Medical Center	March 16 2022	Not Applicable

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