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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 |
| Related Syk Products |
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| R-406
R406 is an orally bioavailable and selective inhibitor of spleen tyrosine kinase (Syk) with the IC50 of 41nM and Ki value of 30 nM. |
| Fostamatinib
Fostamatinib (R788) is a spleen tyrosine kinase (Syk) inhibitor with IC50 of 41 nM. |
| P505-15 hydrochloride
P505-15 (PRT062607) is a novel, highly selective inhibitor of Syk with IC50 value of 1-2 nM. |
| GS-9973
GS-9973 is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM. |
| Piceatannol
Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn. |
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