Entospletinib (GS-9973)CAS号: 1229208-44-9分子式: C23H21N7O分子量: 411.46描述纯度储存/保存方法别名可溶性/溶解性靶点In vitro(体外研究)In vivo(体内研究)
产品描述 | |
描述 |
GS-9973 is an oral inhibitor of spleen tyrosine kinase (Syk), with potential antineoplastic activity. |
纯度 |
>98%
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储存/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.
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基本信息 | |
别名 |
GS9973, GS 9973, Entospletinib
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可溶性/溶解性 |
DMSO 82 mg/mL warmed (199.29 mM)
Water slightly soluble or insoluble Ethanol slightly soluble or insoluble |
生物活性 | |
靶点 |
Syk
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In vitro(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.
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In vivo(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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分子结构图