货号	规格	价格	上海	北京	珠海	重庆	武汉	购买数量
S54908-1ml促销	10mM in DMSO	￥682.00 ￥612.00 S54908-1ml ￥612.00 现货	10 10	-	-	-	-

货号

规格

价格

上海

北京

珠海

重庆

武汉

购买数量

S54908-1ml促销

10mM in DMSO

￥682.00 ￥612.00

产品描述：

Syk抑制剂;Syk Inhibitors;说明：Entospletinib (GS-9973)是一种口服具有生物活性的，选择性Syk抑制剂，无细胞试验中IC50为7.7 nM。在细胞中，对Syk的选择性比对其他激酶（如Jak2, ckit, Flt3, Ret, KDR）高13-1000倍。;InformationEntospletinib (GS-9973) Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay and showed 13- to >1000-fold cellular selectivity for Syk over other kinases(including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.TargetsSyk (Cell-free assay) 7.7 nMIn vitroGS-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.In vivoGS-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 .Cell Research(from reference)Cell lines：MV-4-11 cells Concentrations：~10 μM Incubation Time：72 hours

靶点：

IC50: 7.7 nM (Syk)

保存条件：

-80℃（运输条件：冰袋低温运输）

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.43 ml	12.152 ml	24.304 ml
5 mM	0.486 ml	2.43 ml	4.861 ml
10 mM	0.243 ml	1.215 ml	2.43 ml
50 mM	0.049 ml	0.243 ml	0.486 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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