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NCI Drug Dictionary


An orally available inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. Upon oral administration of entospletinib, this agent may inhibit the activity of Syk, which inhibits B-cell receptor (BCR) signaling and leads to an inhibition of tumor cell activation, migration, adhesion and proliferation. Syk, a non-receptor cytoplasmic, BCR-associated tyrosine kinase, is expressed in hematopoietic tissues and is often overexpressed in hematopoeitic malignancies. Check for active clinical trials or closed clinical trials using this agent.
Synonyms:spleen tyrosine kinase inhibitor GS-9973
SYK inhibitor GS-9973
Code name:GS-9973
Chemical structure:6-(1H-indazol-6-yl)-N-(4-(morpholin-4-yl)phenyl)imidazo(1,2-a)pyrazin-8-amine