Apilimod (STA-5326) mesylate

Catalog No.S0785

For research use only.

Apilimod (STA-5326) mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod mesylate (STA-5326 mesylate) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.

Apilimod (STA-5326) mesylate Chemical Structure

CAS No. 870087-36-8

Selleck's Apilimod (STA-5326) mesylate has been cited by 1 Publication

Purity & Quality Control

Choose Selective Interleukins Inhibitors

Biological Activity

Description Apilimod (STA-5326) mesylate is a potent and orally-available inhibitor of the cytokines interleukin-12 (IL-12) and interleukin-23 (IL-23) with the potential to treat certain autoimmune and inflammatory diseases. Apilimod mesylate (STA-5326 mesylate) inhibits IL-12 with IC50 of 1 nM, 1 nM and 2 nM, in IFN-γ/SAC-stimulated human PBMCs, human monocytes and mouse PBMCs, respectively. Apilimod mesylate (STA-5326 mesylate) is also a cell permeable small molecule that specifically inhibits PIKfyve with IC50 of 14 nM.
Targets
IL-12 [1]
(in IFN-γ/SAC-stimulated human PBMCs)
IL-12 [1]
(in human monocytes)
IL-12 [1]
(in mouse PBMCs)
PIKfyve [2]
(Cell-free assay)
1 nM 1 nM 2 nM 14 nM

Protocol (from reference)

Solubility (25°C)

In vitro

Water 100 mg/mL
(163.74 mM)
DMSO 60 mg/mL
(98.24 mM)
Ethanol ''2.5 mg/mL

* 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 610.7
Formula

C25H34N6O8S2

CAS No. 870087-36-8
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CC1=CC(=CC=C1)C=NNC2=CC(=NC(=N2)OCCC3=CC=CC=N3)N4CCOCC4.CS(=O)(=O)O.CS(=O)(=O)O

In vivo Formulation Calculator (Clear solution)

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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
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Molarity Calculator

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00234741 Completed Drug: STA-5326 mesylate Crohn''s Disease Synta Pharmaceuticals Corp.|National Institute of Allergy and Infectious Diseases (NIAID)|National Institutes of Health (NIH) November 2005 Phase 2

(data from https://clinicaltrials.gov, updated on 2021-09-06)

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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