Sertindole

SKU: orb1220662

Description

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.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 106516-24-9
• MW: 440.94
• Purity: >98% (HPLC)
• Formula: C₂₄H₂₆ClFN₄O
• SMILES: Fc1ccc(cc1)-n1cc(C2CCN(CCN3CCNC3=O)CC2)c2cc(Cl)ccc12
• Target: Dopamine Receptor
• Solubility: DMSO:50 mg/mL (113.39 mM)

Bioactivity

• In Vivo:
  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.
  Read more...
• 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. Cell Proliferation Assay Cell 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 μM Incubation 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 0.01).
  Read more...

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Lu 23-174

Quick Database Links

Gene Symbol

Dopamine Receptor