产品描述
Quinacrine is a compound that is commonly used as an anti-protozoal agent. It inhibits voltage-dependent sodium channels (IC50: 3.3 μM) and suppresses aldehyde oxidase (IC50: 3.3 μM). Quinacrine prevents misfolding of prion protein (EC50: 0.3 μM). As an effective riboflavin antagonist, quinacrine associates with the riboflavin-binding protein (Ki: 6.7 μM). Voltage-dependent sodium channels play a vital role in action potential initiation and propagation in excitable cells, including muscle, nerve, and neuroendocrine cell types.
体外活性
Quinacrine, in a dose-dependent manner, effectively reversed the resistance in the multi-drug resistance (MDR) K562 cells. Quinacrine displayed strong toxicity to the MDR K562 cells at a concentration of 10.0 μM. Compared to the control, quinacrine significantly increased the activity of caspase-9 and -3 activities in the MDR K562 and K562 cells in a dose-dependent fashion [1].
体内活性
Female BALB/c nude mice, bearing MDR K562 cell xenografts, were injected with quinacrine at a dose of 10 mg/kg via tail vein for 13 days. Compared to the control group, quinacrine inhibited tumor growth obviously in the treated groups. Furthermore, quinacrine enhanced the anti-tumor effects of vincristine [1].
Cas No.
T23210
分子式
C23H30ClN3O·2HCl [XH2O]
分子量
472.9
别名
Quinacrine (hydrochloride hydrate) (83-89-6 free base)
储存和溶解度
H2O:≥18.65mg/mL
Powder: -20°C for 3 years
In solvent: -80°C for 2 years