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Fostamatinib disodium (R788, R-935788) is a potent, ATP-competitive and selective Syk (Spleen tyrosine kinase) inhibitor with IC50 of 41 nM. It is an orally available disodium salt of the Syk kinase inhibitor fostamatinib with potential anti-inflammatory and immunomodulating activities. Syk kinase, widely expressed in hematopoietic cells, is a nonreceptor tyrosine kinase that is involved in coupling activated immunoreceptors to signal downstream events that mediate diverse cellular responses, including proliferation, differentiation, and phagocytosis. Fostamatinib disodium (R788) inhibits tumor growth in the Eμ- TCL1 transgenic mouse model of CLL by blocking antigen-dependent B-cell receptor signaling. It effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolonged survival of the treated animals. The growth-inhibitory effect of Fostamatinib disodium occurs despite the relatively modest cytotoxic effect in vitro and is independent of basal Syk activity, suggesting that Fostamatinib disodium (R788) functions primarily by inhibiting antigen-dependent BCR signals. Importantly, the effect of Fostamatinib disodium was found to be selective for the malignant clones, as no disturbance in the production of normal B lymphocytes was observed.
J Inflamm Res. 2024 Nov 25;9757-9771.
Fostamatinib, a Spleen Tyrosine Kinase Inhibitor, Exerts Anti-Inflammatory Activity via Inhibiting STAT1/3 Signaling Pathways
Fostamatinib disodium purchased from AbMole
Molecular Weight | 624.42 |
Formula | C23H24FN6O9PNa2 |
CAS Number | 1025687-58-4 |
Solubility (25°C) | DMSO 18 mg/mL (ultrasonic and warming) |
Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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