[CAS NO. 541550-19-0] Apilimod (STA-5326)

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PRODUCTS SPECIFICATIONS [541550-19-0]

Catalog

SLK-S6414

Brand

Selleck

CAS

541550-19-0

DESCRIPTION [541550-19-0]

Overview

MDL	MFCD09954108
Molecular Weight	418.49
Molecular Formula	C23H26N6O2
SMILES	N(N=CC1=CC(C)=CC=C1)C2=CC(=NC(OCCC3=CC=CC=N3)=N2)N4CCOCC4

For research use only.

Storage

3 years,-20°C,powder
1 years,-80°C,in solvent

Shipping

Room temperature shipping(Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Concentration Volume Mass	1 mg	5 mg	10 mg
1 mM	2.3895 mL	11.9477 mL	23.8954 mL
5 mM	0.4779 mL	2.3895 mL	4.7791 mL
10 mM	0.2390 mL	1.1948 mL	2.3895 mL
50 mM	0.0478 mL	0.2390 mL	0.4779 mL

Description

Apilimod (STA-5326) is a potent and orally-available inhibitor of the cytokines and with the potential to treat certain autoimmune and inflammatory diseases. Apilimod (STA-5326) 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 (STA-5326) is also a cell permeable small molecule that specifically inhibits 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 ^[1]
1 nM	1 nM	2 nM	14 nM

In vitro

Apilimod selectively inhibits TLR-induced cytokine expression. It selectively inhibits the production of IL12p40, whereas it has little effect on IL8 production in THP-1 cells.Apilimod reduces not only PtdIns(3,5)P production but also that of PtdIns5P in intact cells.

References

[1] Cai X, et al. Chem Biol. 2013, 20(7):912-21.
[2] Diego Sbrissa, et al. PLoS One. 2018, 13(9): e0204532.
[3] Yumiko Wada, et al. Blood. 2007 Feb 1;109(3):1156-64.
[4] Gayle S, et al. Blood. 2017 Mar 30;129(13):1768-1778.

Synonyms

Benzaldehyde, 3-methyl-, 2-[6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone

Benzaldehyde, 3-methyl-, [6-(4-morpholinyl)-2-[2-(2-pyridinyl)ethoxy]-4-pyrimidinyl]hydrazone

Apilimod

STA 5326