纯度:>98% by TLC, NMR Conforms
分子式:C19H25NO
分子量:319.87
溶剂:DMSO (30 mg/ml) Water (75 mg/ml)
性状:White solid
存储:-20°C
Activity (short version):Anti-estrogen, Chemo-potentiating agent
Function / Pharmacology:Tesmilifene, an analog of tamoxifen, acts as a chemopotentiator and antineoplastic agent and was developed for the treatment of breast cancer but never marketed.1 It binds with high affinity to the anti-estrogen binding site (AEBS) in rat liver microsomes but does not bind to the estrogen receptor (at or below 10 μM) .2 Displaces histamine from AEBS, an activity which correlates with its cytotoxic effects on breast cancer cells.2 Enhances the cytotoxicity of taxol, epirubicin, doxorubicin and vinorelbine in multidrug resistance cell lines.3 It has been shown to increase the permeability of the blood-brain and blood-glioma barrier in culture and animal models by modifying brain endothelial functions.4