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Syk Inhibitor II dihydrochloride

产品编号 T4391 CAS 227449-73-2

别名: Syk Inhibitor II (hydrochloride)

Syk Inhibitor II (hydrochloride) 是一种非受体酪氨酸激酶，磷酸化后，它与 FcRγ 链的基于免疫受体酪氨酸的激活基序结合，并介导与血小板功能和炎症相关的下游信号传导。 Syk inhibitor II 是一种可渗透细胞的嘧啶-甲酰胺化合物，以 ATP 竞争性方式选择性和可逆地阻断 Syk (IC50 = 41 nM)。它对 PKCε、PKCβII、ZAP-70、Btk 和 Itk 的效力要低得多（IC50s 分别为5.1、11、11.2、15.5 和 22.6 μM）。

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Syk Inhibitor II dihydrochloride Chemical Structure

Syk Inhibitor II dihydrochloride, CAS 227449-73-2

规格	价格/CNY	货期
1 mg	￥ 1,270	现货
2 mg	￥ 2,150	现货
5 mg	￥ 3,650	现货
10 mg	￥ 5,260	现货
25 mg	￥ 8,170	现货
50 mg	￥ 10,800	现货
100 mg	￥ 14,800	现货
1 mL * 10 mM (in DMSO)	￥ 4,630	现货

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其他形式的 Syk Inhibitor II dihydrochloride:

Syk Inhibitor II
现货
Syk Inhibitor II hydrochloride
现货
Syk Inhibitor II dihydrochloride dihydrate
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生物活性

化学信息

存储 & 溶解度

参考文献

相关产品

产品描述	Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that, upon phosphorylation, binds to immunoreceptor tyrosine-based activation motifs of FcRγ chains and mediates downstream signaling related to platelet function and inflammation. Syk inhibitor II is a cell-permeable, pyrimidine-carboxamide compound that selectively and reversibly blocks Syk (IC50 = 41 nM) in an ATP-competitive manner. It is much less potent against PKCε, PKCβII, ZAP-70, Btk, and Itk (IC50s = 5.1, 11, 11.2, 15.5, and 22.6 μM, respectively).
靶点活性	BTK:15.5 μM, ZAP70:11.2 μM, PKCε:5.1 μM, PKCβII:11 μM, Syk:41 nM, ITK:22.6 μM
体外活性	Syk inhibitor II has been shown to prevent FcεRI-mediated 5-HT release in RBL-2H3 cells in vitro (IC50 = 460 nM).
体内活性	Syk inhibitor II has been shown to inhibit passive cutaneous anaphylaxis reactions in mice (ID50 = 13.2 mg/kg, s.c.).
激酶实验	A 2 μM portion of DMSO solution of each compound to be tested was added to each well containing 50 ll of a reaction solution [composition: 20–200 ng of recombinant kinase, 50 mM Tris–HCl (pH 7–8), 10 mM MgCl2 or MnCl2, 50 mM NaCl, 1 mM DTT, optimum concentration of the substrate peptide, and 0.1 lCi [c 33P]ATP (10 mCi/mL, Amersham)]. This was prepared in OptiplateTM (PACKARD) and allowed to stand at room temperature for 1 h to effect tyrosine phosphorylation. The reaction was terminated by adding PBS containing 0.25 mg SPA beads, 50 lM ATP, 5 mM EDTA, and 1% Triton X-100 in an amount of 150 ll per well. The plate was sealed, stirred, allowed to stand at room temperature for 15 min, and then centrifuged at 1500 rpm for 3 min to effect precipitation of the SPA beads. Radioactivity of each well was measured using TOP COUNT (PACKARD), and the tyrosine phosphorylation activity by the kinases was calculated. They are for reference only.
动物实验	ICR mice were passively sensitized by subcutaneously injectinganti-dinitrophenyl (DNP)-coupled IgE under the right ear pinna, while lightly anesthetizing with ether. After 24hr, each mouse was challenged by injecting amixture of DNP-conjugated bovine serum albumin and 200 μl of 0.5% Evans blue solution via the tail vein to induce passive cutaneous anaphylaxis. Thirty minutes after the challenge, the mice were sacrificed to take both ears and the amount of dye from the blueing region was measured. Test compounds or vehicle alone as a control were subcutaneously administered to the mice 30 minbefore the antigen challenge. The dye in the tissues was extracted with formamide and colorimetrically determined at 620 nm. A value obtained by subtracting the dye content of the left ear from the dye content of the right ear was used as the amount of dye leaked into the tissues by the PCA reaction.

别名	Syk Inhibitor II (hydrochloride)
分子量	413.22
分子式	C14H17Cl2F3N6O
CAS No.	227449-73-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

溶解度

PBS(pH7.2): 10 mg/mL

Ethanol: 0.3 mg/mL

DMSO: 30 mg/mL

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

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参考文献

1. Hisamichi H, etal. Synthetic studies on novel Syk inhibitors. Part 1: Synthesis and structure–activity relationships of pyrimidine-5-carboxamide derivatives[J]. Bioorganic & medicinal chemistry, 2005, 13(16): 4936-4951.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +

% Tween 80+

% ddH₂O

%DMSO+

计算重置

计算结果如下:

工作液浓度: mg/ml;

母液配置方法: mg 药物溶于 μL DMSO (母液浓度为 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 μL DMSO 主液，加入 μL PEG300，混匀澄清，再加 μL Tween 80，混匀澄清，再加 μL ddH₂O, 混匀澄清。

备注:

要按顺序从左向右依次添加助溶剂。可配合物理方法，如涡流、超声波或热水浴使之帮助溶解。

技术支持

您可能有的问题的答案可以在抑制剂处理说明中找到，包括如何准备库存溶液，如何存储产品，以及基于细胞的分析和动物实验需要特别注意的问题。

Keywords

Syk Inhibitor II dihydrochloride 227449-73-2 Angiogenesis Chromatin/Epigenetic Cytoskeletal Signaling Others Tyrosine Kinase/Adaptors Tyrosine Kinases Syk PKC BTK Syk Inhibitor II Syk Inhibitor II (hydrochloride) Syk Inhibitor II Dihydrochloride Inhibitor inhibitor inhibit

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Syk Inhibitor II dihydrochloride

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参考文献

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