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Tie2 kinase inhibitor 1

Tie2 kinase inhibitor 1

产品编号 T6335   CAS 948557-43-5
别名: Tie2 kinase inhibitor

Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor) 是Tie2激酶选择性抑制剂9IC50:250 nM),具有抗癌作用。

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Tie2 kinase inhibitor 1 Chemical Structure
Tie2 kinase inhibitor 1, CAS 948557-43-5
规格 价格/CNY 货期 数量
1 mg ¥ 552 现货
2 mg ¥ 803 现货
5 mg ¥ 1,720 现货
10 mg ¥ 2,570 现货
25 mg ¥ 4,450 现货
50 mg ¥ 6,680 现货
100 mg ¥ 8,830 现货
500 mg ¥ 17,800 现货
1 mL * 10 mM (in DMSO) ¥ 1,720 现货
产品目录号及名称: Tie2 kinase inhibitor 1 (T6335)
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生物活性
化学信息
存储 & 溶解度
参考文献
产品描述 Tie2 kinase inhibitor 1 (Tie2 kinase inhibitor), an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.
靶点活性 Tie-2:0.25 μM
体外活性 In HEL cells, Tie2 kinase inhibitor(IC50=232 nM) displays medium cellular activities. Tie2 kinase inhibitor 1 shows a medium inhibitory activity against Tie2 tyrosine kinase 1. Tie2 kinase inhibitor 1 is more specific for Tie2 than p38 (IC50=50 μM), and is a >10-fold specificity than VEGFR2, VEGFR3, and PDGFR1β.
体内活性 In a matrigel mouse model of angiogenesis, Tie2 kinase inhibitor 1 reduces angiogenesis. At doses of 25 and 50 mg/kg (i.p., b.i.d) for Tie2 kinase inhibitor, results on a reduction of 41% and 70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor 1 treatment results in a modest dose-dependent delay in tumor growth.
激酶实验 Enzymatic HDAC activity assays: 40 μL enzyme buffer (15 mM Tris HCl pH 8.1, 0.25 mM EDTA, 250 mM NaCl, 10% v:v glycerol) containing HDAC1, 3, 6 or 8 activity, 29 μL enzyme buffer and 1 μL resminostat at different concentrations are added to a 96-well microtitre plate and the reaction started by the addition of 30μL substrate peptide Ac-NH-GGK(Ac)-AMC (HDAC1, 3 and 6 assays, final concentrations 6 μM for HDAC1, 10 μM for HDAC6 and 25 μM for HDAC3/DAD) or Ac-RHK(Ac)K(Ac)-AMC (HDAC8 assay, final concentration 50 μM). After incubation for 3 hours (HDAC1, HDAC6, HDAC8) or 2 hours (HDAC3) at 30°C, the reaction is terminated by the addition of 25 μL stop solution (50 mM Tris HCl pH 8, 100 mM NaCl, 0.5 mg/mL trypsin and 2 μM trichostatin A [TSA]). After incubation at room temperature for further 40 min, fluorescence is measured using a multilabel counter (extinction 355 nm, emission 460 nm) for quantification of AMC generated by tryptic cleavage of the deacetylated peptide. For the calculation of the IC50, the fluorescence in wells without test compound (1% DMSO, negative control) is set as 100% enzymatic activity and the fluorescence in wells with 2 μM TSA (positive control) is set at 0% enzymatic activity (background fluorescence substracted).
动物实验 In MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor 1(≤50 mg), which is dissolved in 5% EtOH+5%cremophor+90% water, is injected intraperitoneally.
别名 Tie2 kinase inhibitor
分子量 439.53
分子式 C26H21N3O2S
CAS No. 948557-43-5

存储

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

溶解度

DMSO: 33 mg/mL (75.1 mM)

Ethanol: < 1 mg/mL (insoluble or slightly soluble)

H2O: < 1 mg/mL (insoluble or slightly soluble)

溶液配制表

可选溶剂 浓度 体积 质量 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.2752 mL 11.3758 mL 22.7516 mL 56.8789 mL
5 mM 0.455 mL 2.2752 mL 4.5503 mL 11.3758 mL
10 mM 0.2275 mL 1.1376 mL 2.2752 mL 5.6879 mL
20 mM 0.1138 mL 0.5688 mL 1.1376 mL 2.8439 mL
50 mM 0.0455 mL 0.2275 mL 0.455 mL 1.1376 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
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参考文献

1. Semones M, et al. Bioorg Med Chem Lett, 2007, 17(17), 4756-4760.
Pexmetinib TIE-2/VEGFR-2 kinase-IN-5 CE-245677 EOC317 Altiratinib BAY-826 Foretinib GSK-1070916

相关化合物库

该产品包含在如下化合物库中:
抗癌活性化合物库 酪氨酸激酶分子库 高选择性抑制剂库 已知活性化合物库 表型筛选靶点鉴定库 经典已知活性库 抗癌化合物库 抑制剂库 NO PAINS 化合物库 激酶抑制剂库

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
g
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
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% Tween 80
% ddH2O
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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

Tie2 kinase inhibitor 1 948557-43-5 Tyrosine Kinase/Adaptors Tie-2 internal Tie2 tumor Tie2 kinase inhibitor anti-cancer kinase inhibit Tie-2 kinase inhibitor 1 Inhibitor tunica endothelial inhibitor

 

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