Sertindole

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

Sertindole (Lu 23-174) 是一种具有口服活性的 5-HT2A、5-HT2C、dopamine D2、和 αl-adrenergic 受体拮抗剂。Sertindole 表现出对多种癌症细胞的抗增殖活性并可用于抗精神病的研究。

Sertindole is an atypical antipsychotic that binds to dopamine D2 receptors and the serotonin (5-HT) receptor subtypes 5-HT1D 5-HT2A and 5-HT2C (Kds = 2.7 20 0.14 and 6 nM respectively)(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.(In Vivo):Sertindole (oral gavage; 10?mg/kg; once daily; 12 d) shows anti-tumor activity in vivo.

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. Cell Proliferation AssayCell Line:SUM159 and MCF-10A cells Concentration:0-100 μM Incubation Time:48 hours Result:Showed IC50s of 9.2?μM and 27.6?μM for SUM159 and MCF-10A cells, respectively.Cell Proliferation Assay Cell Line:NCI-H460, A549, NCI-H446, NCI-H661, 801-D, U251, A172, U118-MG, U87-MG, AGS, MKN45, BGC-823, SGC-7901, HT-29, COLO205, SW480, SW620, HCT-15, HepG2, Bel-7402, MCF-7, MDA-MB-231, SUM159, T47D, MDA-MB-453, ZR-75-1, CCRF-CEM, K562, Jurkat, MCF-10A cells Concentration:0.8-27.6 μMIncubation Time:48 hours Result:Showed IC50s ranging between 0.8-12.7?μM, 2.7-4.6?μM, 12.7-15.3?μM and 8.6-16.1?μM for breast cancer, leukemia, hepatoma and glioblastoma lines, respectively.Cell Migration Assay Cell Line:SUM159 cells Concentration:5?μΜ and 10 μΜ Incubation Time:24 hours Result:Blocked around 50% cells traversing the membranes at 5?μΜ, and almost all the cells lost traversing ability at 10?μΜ.Elevated LC3II conversion significantly (P?

Sertindole (oral gavage; 10?mg/kg; once daily; 12 d) shows anti-tumor activity in vivo. Animal Model:Immune-deficient Balb/c mice implanted MDA-MB-231 human TNBC cells Dosage:10?mg/kg Administration:Oral gavage; 10?mg/kg; once daily; 12 days Result:Exhibited a 22.7% reduction in size after a 12-day administration regimen.

Lu 23-174

GPCR/G Protein

Dopamine Receptor

D2|5-HT

Metabolic Disease

Chronic obstructive pulmonary disease

106516-24-9

440.94

C24H26ClFN4O

>98% (HPLC)

DMSO:50 mg/mL (113.39 mM)

Fc1ccc(cc1)-n1cc(C2CCN(CCN3CCNC3=O)CC2)c2cc(Cl)ccc12

1-[2-[4-[5-chloro-1-(4-fluorophenyl)indol-3-yl]piperidin-1-yl]ethyl]imidazolidin-2-one

(-20℃)

With Ice Pack

≥ 2 years