Apilimod dimesylate

Name: Apilimod dimesylate
Brand: Tocris Bioscience
SKU: 7283

Tocris Bioscience, part of Bio-Techne | Catalog # 7283

Citations (6)

COA / SDS

Potent and selective PIKfyve inhibitor

Key Product Details

Description:	Potent and selective PIKfyve inhibitor
Chemical Name:	4-(6-(2-(3-Methylbenzylidene)hydrazinyl)-2-(2-(pyridin-2-yl)ethoxy)pyrimidin-4-yl)morpholine dimethanesulfonate
Purity:	≥98% (HPLC)
Molecular Weight:	610.7

View Full Technical Details for Apilimod dimesylate

Technical Data
Citations

Biological Activity for Apilimod dimesylate

Apilimod dimesylate is a potent and selective PIKfyve inhibitor (IC₅₀ = 14 nM). Exhibits no significant activity at other lipid kinases and protein kinases, including PIP4K, PIP5K, mTOR, PI3K and PI4K. Inhibits cellular entry by SARS-CoV-2, MERS-CoV and MHV S pseudovirions. Apilimod dimesylate reduces the number of SARS-CoV-2-infected hiPSC-derived pneumocyte-like cells by 85% and inhibits SARS-CoV-2 replication in donor lung tissue. Also exhibits selective cytotoxicity in B-cell non-Hodgkin lymphoma compared with normal cells. Inhibits production of IL-12 and IL-23. In motor neurons derived from patients with amyotrophic lateral sclerosis (ALS) Apilimod dimesylate promotes exocytosis of neurotoxic proteins and in mouse ALS models, the compound reduces pathology and prolongs survival. Anti-inflammatory. Water-soluble.

Compound Libraries for Apilimod dimesylate

Apilimod dimesylate is also offered as part of the Tocriscreen 2.0 Max and Tocriscreen Kinase Inhibitor Library. Find out more about compound libraries available from Tocris.

Technical Data for Apilimod dimesylate

M. Wt	610.7
Formula	C₂₃H₂₆N₆O₂.2CH₃SO₃H
Storage	Store at -20°C
Purity	≥98% (HPLC)
CAS Number	870087-36-8
PubChem ID	91885471
InChi Key	GAJWNIKZLYZYSY-OKUPSQOASA-N
Smiles	C[S](O)(=O)=O.C[S](O)(=O)=O.CC1=CC=CC(\C=N\NC2=CC(=NC(OCCC3=CC=CC=N3)=N2)N2CCOCC2)=C1

The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.

Tocris products are intended for laboratory research use only, unless stated otherwise.

Solubility for Apilimod dimesylate

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	water	61.07	100
	DMSO	30.53	50

Preparing Stock Solutions for Apilimod dimesylate

The following data is based on the product molecular weight 610.7.

Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.64 mL	8.19 mL	16.37 mL
5 mM	0.33 mL	1.64 mL	3.27 mL
10 mM	0.16 mL	0.82 mL	1.64 mL
50 mM	0.03 mL	0.16 mL	0.33 mL

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References for Apilimod dimesylate

References are publications that support the biological activity of the product.

Hung PIKFYVE inhibition mitigates disease in models of diverse forms of ALS. Cell 2023 PMID: 36754049
Gayle Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 2017 PMID: 28104689
Ou Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 2020 PMID: 32221306
Riva Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature 2020 PMID: 32707573
Cai PIKfyve, a class III PI-kinase, is the target of the small molecular IL12/23 inhibitor apilimod and a new player in toll-like receptor signaling. Chem.Biol. 2013 PMID: 23890009
Wada Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 2007 PMID: 17053051