Fostamatinib disodium | Syk inhibitor

CAS:
 1025687-58-4
Catalog Number:
 10-4144
Fostamatinib disodium chemical structure

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5 mg$80.00
25 mg$275.00

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

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
CAS:
1025687-58-4
Catalog Number:
10-4144
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

Safety Data Sheet:

Product Data Sheet:

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