Fostamatinib disodium | Syk inhibitor

CAS:1025687-58-4

Catalog Number:10-4144

Fostamatinib disodium (1025687-58-4) is a prodrug of the spleen tyrosine kinase inhibitor (Syk) R406 and is approved 

for the treatment of chronic immune thrombocytopenia.  It has demonstrated significant reduction in inflammatory 

mediators such as TNFα, IL-1, IL-6, and IL-8 in arthritis models.1  Syk IC50 = 41 nM – Fostamatinib also inhibits Flt3, 

Lyn, and Lck with similar potency in vitro but displays higher selectivity Syk in cellular assays.2 Significantly inhibits 

LPS-induced inflammatory response via blocking STAT1/3 signaling.3 Fostamatinib restored myeloid homeostasis in 

severe COVID-19.4 Displayed synergistic effects with anti-PDL1 therapy against neuroblastoma.5 Fostamatinib induces 

metabolic reprogramming of acute myeloid leukemia stem cells.6

Activity:Syk inhibitor

Chemical Names:

[6-[[5-Fluoro-2-(3,4,5-trimethoxyanilino)pyrimidin-4-yl]amino]-2,2-dimethyl-3-oxopyrido[3,2-b][1,4]oxazin-4-yl]methyl 

phosphate Disodium salt

Alternate Name:R788

Molecular Weight:624.43

Molecular Formula:C23H24FN6O9P·2Na

Solubility:Soluble in DMSO (12 mg/ml with warming)

Physical Properties:White solid

Purity:>98% HPLC

NMR: (Conforms)

Storage Temperature:-20°C

Stability:Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:RT

References/Citations:

1.Bajpai et al. (2009), Fostamatinib, a Syk inhibitor prodrug for the treatment of inflammatory diseases; iDrug 12 174

2.McAdoo and Tam (2011), Fostamatinib Disodium; Drugs Future 36 273

3.Guo et al. (2024), Fostamatinib, a Spleen Tyrosine Kinase Inhibitor, Exerts Anti-Inflammatory Activity via Inhibiting STAT1/3 

Signaling Pathways; J. Inflamm. Res. 17 9757

4.Wigerblad et al. (2023), Spleen tyrosine kinase inhibition restores myeloid homeostasis in COVID-19; Sci. Adv. 9 eade8272

5.Rohila et al. (2023), Targeting macrophage Syk enhances responses to immune checkpoint blockade and radiotherapy in 

high-risk neuroblastoma; Front. Immunol. 14 1148317

6.Polak et al. (2020), SYK inhibition targets acute myeloid leukemia stem cells by blocking their oxidative metabolism;

 Cell Death Dis. 11 956