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Entospletinib

CAS No. : 1229208-44-9

MCE 国际站：Entospletinib

产品活性：Entospletinib (GS-9973) 是一种可口服，选择性的 Syk 抑制剂，IC₅₀ 值为 7.7 nM。

研究领域：Protein Tyrosine Kinase/RTK

作用靶点：Syk

In Vitro: Entospletinib (GS-9973) shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, 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.
The combination of idelalisib and Entospletinib (GS-9973) synergistically inhibits CLL cell viability and further disrupts chemokine signaling.

In Vivo: Entospletinib (GS-9973) (1 mg/kg, p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, Entospletinib (GS-9973) (1-10 mg/kg, p.o.) significantly inhibits ankle inflammation. Moreover, Entospletinib (GS-9973) also shows disease-modifying activity in multiple histological measurements, including inhibition of pannus formation, cartilage damage, bone resorption, and peritosteal bone formation with ED₅₀ ranging from 1.2 to 3.9 mg/kg.

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