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Description: Fostamatinib (also known as R788; trade name: Tavalisse), a prodrug of the active metabolite R406, is an orally bioactive, potent and selective Syk inhibitor with IC50 of 41 nM in a cell-free assay. On 4/17/2018, Fostamatinib was approved by FDA to treat thrombocytopenia in adult patients with persistent or chronic immune thrombocytopenia (ITP). Fostamatinib strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Fostamatinib has displayed anti-inflammatory and immunomodulating activities. Fostamatinib inhibits Syk kinase-mediated IgG Fc gamma receptor signaling, resulting in inhibition of the activation of mast cells, macrophages, and B-cells and related inflammatory responses and tissue damage.
References: Blood. 2010 Dec 2; 116(23):4894-905.
Related CAS#:1025687-58-4 (sodium); 901119-35-5 (free)
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