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抑制剂描述:

产品名称:Entospletinib (GS-9973)

产品别名:见爱必信官网

英文别名:Entospletinib (GS-9973)

靶点:Syk

CAS:1229208-44-9

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

GS-9973 is an oral inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity.

溶解性:DMSO 82 mg/mL warmed (199.29 mM)
Water slightly soluble or insoluble
Ethanol slightly soluble or insoluble

体外研究:

GS-9973 shows good bidirectional permeability across Caco-2 cell monolayers in vitro. In cells, 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 GS-9973 synergistically inhibits CLL cell viability and further disrupts chemokine signaling.

体内研究:GS-9973 (1 mg/kg p.o.) shows moderate to high bioavailability in rat and dog. In a rat collagen-induced arthritis model, GS-9973 (1-10 mg/kg p.o.) significantly inhibits ankle inflammation. Moreover, 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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