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Fostamatinib (R788) is a precursor of the active compound tamatinib (R-406), which is an inhibitor of the enzyme spleen tyrosine kinase (Syk). R788 (Fostamatinib) 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. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8 and GM-CSF. R788 (Fostamatinib) induces apoptosis of the majority of examined DLBCL cell lines.
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Source | Blood (2010). Figure 2.R788 |
| Method | apoptosis assay | |
| Cell Lines | TCL1 leukemia cells | |
| Concentrations | 10 μM | |
| Incubation Time | 24, 48, and 72 h | |
| Results | As shown in Figure 2, a modest decrease in the percentage of viable (annexin V/PI negative) cells was observed at the highest R406 concentrations. |
| Cell Experiment | |
|---|---|
| Cell lines | Cultured human mast cells (CHMC) |
| Preparation method | Human Mast Cell Culture and Stimulation. Cultured human mast cells (CHMC) were derived from cord blood CD34+ progenitor cells and grown, primed, and stimulated as described previously (Rossi et al., 2006) and shown in supplemental data. Before stimulation, cells were incubated with R406 or DMSO for 30 min. Cells were then stimulated with either 0.25 to 2 mg/ml anti-IgE or anti-IgG or 2 μM ionomycin. For tryptase measurement, ∼1500 cells per well were stimulated for 30 min in modified Tyrode's buffer. For LTC4 and cytokine production, 100,000 cells per well were stimulated for 1 or 7 h, respectively. Tryptase activity was measured by luminescence readout of a peptide substrate, and LTC4 and cytokines were measured using Luminex multiplex technology. |
| Concentrations | 0~20 μM |
| Incubation time | 30 min |
| Animal Experiment | |
|---|---|
| Animal models | K/BxN Model Arthritis induced in C57BL/6 mice |
| Formulation | 35% TPGS, 60% PEG 400, and 5% propylene glycol |
| Dosages | 5 and 10mg/kg b.i.d for 13 days |
| Administration | orally |
| Molecular Weight | 580.46 |
| Formula | C23H26FN6O9P |
| CAS Number | 901119-35-5 |
| Solubility (25°C) | DMSO 60 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Syk Products |
|---|
| 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 disodium
Fostamatinib disodium (R788, R-935788) is a potent, ATP-competitive and selective Syk (Spleen tyrosine kinase) 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. Piceatannol is a naturally occurring polyphenolic stilbene found in various fruits and vegetables and exhibits anticancer and anti-inflammatory properties. |
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