Molecular Weight(MW): 580.46
Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.
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B cells were stimulated by irradiated CD40L+ L cells. Forward scatter vs. BrdU incorporation analysis (day 5) in the gated CD19+ CLL cells (D). The distribution of cells with high FSC (blasts, right quadrants) and proliferation (BrdU+, upper quadrants) are shown.
Haematologica, 2016 Feb, 101(2): e59–e62.. Fostamatinib (R788) purchased from Selleck.
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Choose Selective Syk Inhibitors
|Description||Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.|
|Features||Converted into its active metabolite R406 in vivo.|
R788 is a prodrug of the spleen tyrosine kinase (Syk) inhibitor R406. R788 is a competitive inhibitor for ATP binding with a Ki of 30 nM. R788 dose-dependently inhibits anti-IgE-mediated CHMC degranulation with an EC50 of 56 nM. R788 also inhibits the anti-IgE-induced production and release of LTC4 and cytokines and chemokines, including TNFα, IL-8, and GM-CSF. Inhibition of Syk by R788 results in inhibition of all phosphorylation events downstream of Syk signaling. Next to FcϵRI signaling in CHMC, R788 most potently inhibits the signaling of IL-4 and IL-2 receptors. R788 specifically inhibits FcγR signaling in human mast cells, macrophages, and neutrophils. R788 can inhibit local inflammatory injury mediated by immune complexes.  R788 induces apoptosis of the majority of examined DLBCL cell lines. In R788-sensitive DLBCL cell lines, R788 specifically inhibits both tonic- and ligand-induced BCR signaling (autophosphorylation of SYK525/526 and SYK-dependent phosphorylation of the B-cell linker protein [BLNK]). 
|In vivo||Oral administration of R788 to mice reduces immune complex-mediated inflammation in a reverse-passive Arthus reaction and two antibody-induced arthritis models.  In another study, R788 effectively inhibits BCR signaling in vivo, resulting in reduced proliferation and survival of the malignant B cells and significantly prolongs survival of the treated animals.  R788 demonstrates a significant reduction in major inflammatory mediators such as TNFalpha, IL-1, IL-6 and IL-18, leading to reduced inflammation and bone degradation in models of rheumatoid arthritis. |
Fluorescence polarization kinase assay and Ki determination:The fluorescence polarization reactions are performed. For Ki determination, duplicate 200-μL reactions are set up at eight different ATP concentrations from 200 μM (2-fold serial dilutions) in the presence of either DMSO or R788 at 125, 62.5, 31.25, 15.5, or 7.8 nM. At different time points, 20 μL of each reaction is removed and quenched to stop the reaction. For each concentration of R788, the rate of reaction at each concentration of ATP is determined and plotted against the ATP concentration to determine the apparent Km and Vmax (maximal rate). Finally the apparent Km (or apparent Ki/Vmax) is plotted against the inhibitor concentration to determine the Ki.
|In vitro||DMSO||116 mg/mL (199.84 mM)|
|In vivo||4% DMSO+30% PEG 300+ddH2O||5mg/mL|
* 1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
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Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT02612558||Recruiting||Warm Antibody Autoimmune Hemolytic Anemia||Rigel Pharmaceuticals||April 2016||Phase 2|
|NCT02611063||Recruiting||Hematological Malignancies||Stefanie Sarantopoulos, MD, PhD.|Duke University||January 2016||Phase 1|
|NCT02433236||Withdrawn||IGA Nephropathy||Rigel Pharmaceuticals||September 2015||Phase 2|
|NCT02076412||Completed||Immune Thrombocytopenic Purpura||Rigel Pharmaceuticals||November 2014||Phase 3|
|NCT02112838||Recruiting||IGA Nephropathy||Rigel Pharmaceuticals||October 2014||Phase 2|
|NCT02077192||Recruiting||Immune Thrombocytopenic Purpura||Rigel Pharmaceuticals||July 2014||Phase 3|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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