产品
编 号:F384270
分子式:C21H27NO3
分子量:341.44
产品类型
结构图
CAS No: 54063-53-5
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产品详情
生物活性:
Propafenone (SA-79), a sodium-channel blocker, acts an antiarrhythmic agent. Propafenone also has high affinity for the β receptor (IC50=32 nM). Propafenone blocks the transient outward current (Ito) and the sustained delayed rectifier K current (Isus) with IC50 values of 4.9?μm and 8.6?μm, respectively. Propafenone suppresses esophageal cancer proliferation through inducing mitochondrial dysfunction and induce apoptosis.
体内研究:
Propafenone (20 mg/kg; intraperitoneal injection every other day) markedly suppresses the tumor burden with a decrease of 69.2%.Propafenone also significantly inhibits tumor cell proliferation (mean index decreased from 56.3±6.7% in the DMSO-treated group to 20.7±5.1% in the 10 mg/kg propafenone-treated group and 11.3±4.0% in the 20 mg/kg propafenone-treated group).Animal Model:Female BALB/c nude mice bearing KYSE270-derived xenografts (6-8 weeks)
Dosage:10 mg/kg or 20 mg/kg
Administration:Intraperitoneally injected
Result:Exerted a significantly inhibitory effect on the growth of tumor xenografts.
体外研究:
Propafenone (5-25 μM) inhibits esophageal squamous cell carcinoma (ESCC) cell proliferation.Propafenone causes mitochondrial dysfunction by a decreased mitochondrial membrane potential and reduced expression of Bcl-xL and Bcl-2. Propafenone (10 and 20 μm) treatment significantly down regulates the expression levels of the anti-apoptotic proteins Bcl-xL and Bcl-2 in ESCC cells. Propafenone also reduces expression of p-ERK.