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Saracatinib(AZD0530)
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Saracatinib(AZD0530)图片
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
25mg电议
100mg电议

产品介绍
Saracatinib (AZD0530) (AZD0530) 是一种有效的 Src 家族抑制剂,对 c-Src、Lck、c-YES、Lyn、Fyn、Fgr 和 Blk 的 IC50 为 2.7 至 11 nM。 Saracatinib (AZD0530) 显示出比其他酪氨酸激酶高的选择性。

Cell lines

A549 cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37 ℃ for 10 minutes and/or shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Reaction Conditions

1 μM, 24 hours for cell migration inhibition 48 hours for cell invasion inhibition

Applications

A549 cells were grown to confluent monolayers, which were scratched with a pipette tip and incubated with AZD0530 at concentrations ranging from 100 to 1000 nM. DMSO treated control cells continuously migrated into the scratch and nearly closed the scratch within 24 hours. Cell migration was significantly inhibited by AZD0530 in a dose-dependent way. At the highest dose tested (1 μM), AZD0530 reduced A549 cell migration by more than 60%. Cell invasion was tested using a modified Matrigel assay with A549 cells. AZD0530 significantly reduced Matrigel invasion in A549 cells by 51%.

Animal models

Female athymic nude mice injected with Panc410 cells

Dosage form

Oral administration, 50mg/kg/d for 28 days

Applications

AZD0530 administration clearly down-regulated Src, FAK, p-FAK, and pSTAT-3 expression in the sensitive tumor (Panc410) compared with control tumors. In addition, AZD0530 administration resulted in the down-regulation of XIAP as evidenced by the immunoblot of Panc410.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

产品描述

Saracatinib (AZD0530) is a novel, potent Src family kinase (SFK)/Abl dual-kinase inhibitor with IC50 value of 2.7 nM [1].

Saracatinib has been reported to inhibit Src activation in DU145 and PC3 cell lines (prostate cancer cell lines). Both of c-Myc and cyclin D1 expression are decreased by Saracatinib. Saracatinib can inhibit the ERK1/2 and GSK3b phosphorylation as well as decrease β-catenin level in cells. Saracatinib inhibits the prostate tumor cell growth by inducing cycle arrest at G1/S phase. Saracatinib dose-dependently blocks cell migration in DU145 and PC3 cell lines [1].

In DU145 implanted orthotopic SCID mice model, treatment with Saracatinib has been demonstrated to down-regulate the Src expression as well as suppress the tumor size [1].

References:
[1] Chang YM1, Bai L, Liu S, Yang JC, Kung HJ, Evans CP. Src family kinase oncogenic potential and pathways in prostate cancer as revealed by AZD0530. Oncogene. 2008 Oct 23;27(49):6365-75.