货号	规格	价格	上海	北京	珠海	重庆	武汉
S82536-1mg	≥98%	￥358.00 S82536-1mg ￥358.00 现货	10 10	-	-	-	-
S82536-5mg	≥98%	￥944.00 S82536-5mg ￥944.00 现货	10 10	-	-	-	-
S82536-10mg	≥98%	￥1512.00 S82536-10mg ￥1512.00 现货	10 10	-	-	-	-
S82536-25mg	≥98%	￥2376.00 S82536-25mg ￥2376.00 现货	2 2	-	-	-	-
S82536-50mg	≥98%	￥3296.00 S82536-50mg ￥3296.00 现货	4 4	-	-	-	-

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产品描述：

Ilginatinib (NS-018) is a highly active and orally bioavailable JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM).

靶点：

JAK2:0.72 nM (IC50);Tyk2:22 nM (IC50);JAK1:33 nM (IC50);JAK3;39 nM (IC50);TyrosineKinases; JAK

体外研究：

Ilginatinib (NS-018) is a highly active JAK2 inhibitor, with an IC50 of 0.72 nM, 46-, 54-, and 31-fold selectivity for JAK2 over JAK1 (IC50, 33 nM), JAK3 (IC50, 39 nM), and Tyk2 (IC50, 22 nM). Ilginatinib (NS-018) also inhibits Src-family kinases, especially SRC and FYN, and weakly inhibits ABL and FLT3 with 45- and 90-fold selectivity for JAK2, respectively. NS-018 shows potent inhibitory activity against cell lines JAK2V617F or MPLW515L mutations or the TEL-JAK2 fusion gene (expressing a constitutively activated JAK2) with IC50 of 11-120 nM, but has only minimal cytotoxicity against most other hematopoietic cell lines that have no constitutively activated JAK2. Ilginatinib (NS-018) (0.5 μM) preferentially suppresses colony-forming unitgranulocyte/macrophage (CFU-GM) formation from myelodysplastic syndrome (MDS)-derived bone marrow mononuclear cells (BMMNCs). Ilginatinib (NS-018) (1 μM) suppresses the phosphorylation of STAT3 (the downstream kinase of JAK2) in CFU-GM-forming cells from MDS patients

体内研究：

Ilginatinib (NS-018) (12.5, 25, 50, 100 mg/kg, p.o.) potently prolongs the survival of mice and reduces splenomegaly in a mouse Ba/F3-JAK2V617F disease model. Ilginatinib (NS-018) (25, 50 mg/kg, p.o.) significantly reduces leukocytosis, hepatosplenomegaly and extramedullary hematopoiesis, improves nutritional status, and prolongs survival in JAK2V617F transgenic mice

参考文献：

1. Nakaya Y, et al. Efficacy of NS-018, a potent and selective JAK2/Src inhibitor, in primary cells and mouse models of myeloproliferative neoplasms. Blood Cancer J. 2011 Jul;1(7):e29. 2. Kuroda J, et al. NS-018, a selective JAK2 inhibitor, preferentially inhibits CFU-GM colony formation by bone marrow mononuclear cells from high-risk myelodysplastic syndrome patients. Leuk Res. 2014 May;38(5):619-24.

溶解性：

soluble in DMSO

保存条件：

-20℃

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	2.568 ml	12.839 ml	25.679 ml
5 mM	0.514 ml	2.568 ml	5.136 ml
10 mM	0.257 ml	1.284 ml	2.568 ml
50 mM	0.051 ml	0.257 ml	0.514 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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