Apilimod dimesylate

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Cat.No. 7283 - Apilimod dimesylate | C23H26N6O2.2CH3SO3H | CAS No. 870087-36-8
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)
Datasheet
Citations
Reviews
Literature (2)

Biological Activity

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. Reduces 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. Anti-inflammatory. Water-soluble.

Technical Data

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 Data

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

Preparing Stock Solutions

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.

Select a batch to recalculate based on the batch molecular weight:
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

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

Wada et al (2007) Selective abrogation of Th1 response by STA-5326, a potent IL-12/IL-23 inhibitor. Blood 109 1156 PMID: 17053051

Cai et al (2013) 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. 20 912 PMID: 23890009

Riva et al (2020) Discovery of SARS-CoV-2 antiviral drugs through large-scale compound repurposing. Nature PMID: 32707573

Ou et al (2020) Characterization of spike glycoprotein of SARS-CoV-2 on virus entry and its immune cross-reactivity with SARS-CoV. Nat.Commun. 11 1620 PMID: 32221306

Gayle et al (2017) Identification of apilimod as a first-in-class PIKfyve kinase inhibitor for treatment of B-cell non-Hodgkin lymphoma. Blood 129 1768 PMID: 28104689


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