Sertindole (Lu 23-174) is an orally active 5-HT 2A , 5-HT 2C , dopamine D 2 , and αl-adrenergic receptors antagonist. Sertindole shows antipsychotic activity and anti-proliferative activity to multiple cancer cells.
性状
Solid
IC50 & Target[1][2]
5-HT2A Receptor 5-HT2C Receptor
体外研究(In Vitro)
Sertindole (0-100 μM; 48 h) attenuates proliferation of breast cancer cells.Sertindole (0.8-27.6 μM; 48 h) inhibits proliferation toward many cancers in vitro.Sertindole (5?μΜ and 10 μΜ; 24 h) attenuates migration of breast cancer cells. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
Sertindole (oral gavage; 10?mg/kg; once daily; 12 d) shows anti-tumor activity in vivo. has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Model: Immune-deficient Balb/c mice implanted MDA-MB-2
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;4°C 2 years
ClinicalTrial
参考文献
[1]. David Murdoch, et al. Sertindole : a review of its use in schizophrenia. CNS Drugs. 2006;20(3):233-55.[2]. Wei Zhang, et al. Antiproliferative activities of the second-generation antipsychotic drug sertindole against breast cancers with a potential application for treatment of breast-to-brain metastases. Sci Rep. 2018 Oct 25;8(1):15753.
溶解度数据
In Vitro: DMSO : 25 mg/mL (56.70 mM; Need ultrasonic)配制储备液