化合物 Tie2 kinase inhibitor|T6335|TargetMol

Tie2 kinase inhibitor 1
948557-43-5

￥552 1mg 起订

￥1720 5mg 起订

￥2570 10mg 起订

上海更新日期：2024-09-30

TargetMol中国（陶术生物）

VIP3年

联系人：邵小姐

手机：4008200310 拨打

邮箱：marketing@tsbiochem.com

产品详情:

中文名称：: 化合物 Tie2 kinase inhibitor

英文名称：: Tie2 kinase inhibitor 1

CAS号：: 948557-43-5

品牌：: TargetMol

产地：: 美国

保存条件：: Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.

纯度规格：: 99.81%

产品类别：: 抑制剂

货号：: T6335

Product Introduction

Bioactivity

Name	Tie2 kinase inhibitor 1
Description	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.
Kinase Assay	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).
Animal Research	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.
In vitro	在HEL细胞中，Tie2激酶抑制剂（IC50=232 nM）展现出中等的细胞活性。Tie2 kinase inhibitor 1对Tie2酪氨酸激酶1具有中等的抑制效果。Tie2 kinase inhibitor 1对Tie2的特异性很高，并且对VEGFR2、VEGFR3和PDGFR1β的特异性>10倍。
In vivo	在Matrigel小鼠血管生成模型中，Tie2 kinase inhibitor 1能够减少血管生成。当Tie2激酶抑制剂的剂量分别为25 mg/kg和50 mg/kg（i.p.，b.i.d）时，血管生成分别减少了41%和70%。在MOPC-315浆细胞瘤异种移植模型中，Tie2 kinase inhibitor 1的治疗导致肿瘤生长的轻度剂量依赖性延迟。
Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
Solubility Information	DMSO : 4.4 mg/mL (10 mM), Sonication is recommended. Ethanol : < 1 mg/mL (insoluble or slightly soluble) H2O : < 1 mg/mL (insoluble or slightly soluble)
Keywords	internal \| Tie2 \| tumor \| anti-cancer \| kinase \| Tie2 kinase inhibitor 1 \| inhibit \| Tie-2 kinase inhibitor 1 \| Inhibitor \| tunica \| endothelial
Inhibitors Related	GSK-1070916 \| TIE-2/VEGFR-2 kinase-IN-5 \| EOC317 \| CE-245677 \| Altiratinib \| Foretinib \| Pexmetinib \| BAY-826
Related Compound Libraries	Inhibitor Library \| Anti-Cancer Active Compound Library \| Bioactive Compound Library \| Anti-Cancer Compound Library \| Bioactive Compounds Library Max \| Kinase Inhibitor Library \| Highly Selective Inhibitor Library \| NO PAINS Compound Library \| Tyrosine Kinase Inhibitor Library \| Target-Focused Phenotypic Screening Library

Tie2 kinase inhibitor|TargetMol

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿，致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区，已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库，以及多种类型的生化试剂产品，包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等，此外，我们还建设有CADD（计算机辅助药物设计）研究中心、药理实验室、药化合成平台三大技术中心，全方位满足客户的定制需求。凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持，我们将有效帮助您缩短研发周期，取得更成功的结果。

成立日期	(12年)
注册资本	566.265100万人民币
员工人数	100-500人
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