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抑制剂 > 酪氨酸激酶 > Tie2 kinase inhibitor
产品名称:
Tie2 kinase inhibitor
型号:
CS-01Y70007
生产地址
进口、国产
产品价格
电议
产品简介
质量保证、价格优惠
产品详情

一、概述:

化学性质:                                                                                                             

规格

5mg 25mg 100mg

CAS

948557-43-5

别名

N/A

化学名

(S)-4-(4-(6-methoxynaphthalen-2-yl)-2-(4-(methylsulfinyl)phenyl)-1H-imidazol-5-yl)pyridine

分子式

C26H21N3O2S

分子量

439.53

溶解度

22mg/mL in DMSO

储存条件

Store at -20°C

General tips

For obtaining a higher solubility , please warm the tube at 37 and shake it in the ultrasonic bath for a while.

Shipping Condition

Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

 

产品描述:                                                                                                            

IC50: A reversible and selective inhibitor of Tie2 with IC50 of 0.25 M, whose selectivity is 200-fold higher than that of p38.

Genetic studies have identified the crucial roles of Tie receptors (Tie1 & Tie2) in the development and function of endothelial tissues, including promoting the survival, maturation and functional integrity of the vasculature. Tie2 kinase inhibitor is suggested to block vascular construction via suppressing Tie2, and in this way it is expected to disrupt tumor growth and angiogenesis. [1]

In vitro: Tie2 kinase inhibitor exhibited significant inhibitory effect on Tie2 auto-phosphorylation and disrupted its downstream signal transduction in a dose dependent manner in human aortic endothelial cells. In addition, Tie2 kinase inhibitor exhibits moderately suppressed the activity of Tie2 tyrosine kinase in HEL cells with IC50 of 232 nM. [2, 3]

In vivo: Matrigel mouse model of angiogenesis was adopted for in vivo study. Tie2 kinase inhibitor at doses of 25 and 50 mg/kg (i.p., b.i.d) reduced 41% and 70% of angiogenesis, respectively. In a MOPC-315 plasmacytoma xenograft model, Tie2 kinase inhibitor modestly suppressed tumor growth in nude mice in a dose-dependent manner. [4]

Clinical trial: A phase I study was conducted in patients with low or intermediate-1 International Prognostic Scoring System risk MDS to evaluate safety, pharmacokinetics (PK), pharmacodynamics (PD), and preliminary responses of Tie2 kinase inhibitor. It was noticed that this kind of compounds could be well tolerated and has sufficient activity. 1,200 mg once daily was a recommended dose for further study. [5]

特别提醒:                                                                                                              

1. 本产品仅供科研使用。请勿用于医药、临床诊断或治疗,食品及化妆品等用途。请勿存放于普通住宅区。

2. 为了您的安全和健康,请穿好实验服并佩戴一次性手套和口罩操作。

标签:Tie2 kinase inhibitor 

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