Entospletinib (GS-9973) is a potent, selective and orally bioavailable Syk kinase inhibitor with IC50 of 7.7 nM.
Entospletinib (GS-9973) also shows excellent selectivity for Syk, and potently inhibits BCR-mediated activation and proliferation of B-cells as well as immune-complex-stimulated cytokine production in monocytes.
Entospletinib (GS-9973) combined with Idelalisib synergistically inhibits CLL cell viability and further disrupts chemokine signaling.
Entospletinib (GS-9973) (1-10 mg/kg, p.o.) significantly inhibits ankle inflammation in a rat collagen-induced arthritis model, inhibits pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED50 of 1.2-3.9 mg/kg.
