包装 | 价格(元) |
100mg | 电议 |
500mg | 电议 |
1g | 电议 |
5g | 电议 |
Storage | Store at -20°C |
M.Wt | 472.9 |
Formula | C23H30ClN3O·2HCl [XH2O] |
Synonyms | Atebrine,Mepacrine |
Solubility | insoluble in DMSO; ≥18.65 mg/mL in H2O; ≥2.62 mg/mL in EtOH with ultrasonic |
Chemical Name | N4-(6-chloro-2-methoxyacridin-9-yl)-N1,N1-diethylpentane-1,4-diamine, dihydrochloride hydrate |
Canonical SMILES | ClC1=CC=C2C(NC(C)CCCN(CC)CC)=C3C(C=CC(OC)=C3)=NC2=C1.Cl.Cl.O |
运输条件 | 蓝冰运输或根据您的需求运输。 |
一般建议 | 为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存,请尽快用完。 |
IC50: 3.3 μM
Ki = 6.7 μM
Quinacrine, also commonly known as atebrine, is a compound which is commonly used as an anti-protozoal agent. It inhibits voltage-dependent sodium channels with an IC50 value of 3.3 μM and suppresses aldehyde oxidase with an IC50 value of 3.3 μM. Quinacrine prevents misfolding of prion protein with an EC50 value of 0.3 μM. As an effective riboflavin antagonist, quinacrine associates with the riboflavin-binding protein with a Ki value of 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.
In vitro: 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].
In vivo: 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 the tumor growth obviously in the treated groups. Furthermore, quinacrine enhanced the anti-tumor effects of vincristine [1].
Reference:
Liang, G. , Lu, W., Wu, J., Zhao, J., Hong, H., & Long, C. et al. Enhanced therapeutic effects on the multi-drug resistant human leukemia cells in vitro and xenograft in mice using the stealthy liposomal vincristine plus quinacrine. Fundamental & Clinical Pharmacology.2008; 22(4): 429-437.