GS-9973 also known GS9973; GS 9973, cas no:1229208-44-9 is a highly selective and orally efficacious Syk inhibitor(IC50= 7.7 nM) which is currently undergoing clinical evaluation for autoimmune and oncology indications.
IC50 value: 7.7 nM [1]
Target: Syk
The most advanced Syk inhibitor, R406, 1 (or its prodrug form fostamatinib, 2), has shown efficacy in multiple therapeutic indications, but its clinical progress has been hampered by dose-limiting adverse effects that have been attributed, at least in part, to the off-target activities of 1. It is expected that GS-9973 is a more selective Syk inhibitor would provide a greater therapeutic window.
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