包装 | 价格(元) |
10mM (in 1mL DMSO) | 电议 |
5mg | 电议 |
25mg | 电议 |
100mg | 电议 |
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: |