Tesmilifene HCl
Anti-estrogen, Chemo-potentiating agent / 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
Biochemicals & reagents
92981-78-7
BMS-217380-01; YMB1002; DPPE HCl
1 Sorbera et al., (2003), A diphenylmethane derivative specific for the antiestrogen binding site found in rat liver microsomes; Drugs Fut. 28 546 2 Brandes et al., (2008), Tesmilifene hydrochloride; Hum. Exp. Toxicol. 27 143 3 Ferguson et al., (2009), Enhancement of cytotoxicity of natural product drugs against multidrug resistant variant cell lines of human head and neck squamous cell carcinoma and breast carcinoma by temsilifene; Cancer Lett. 274 279 4 Vigushin et al., (2004), Tesmilifene modifies brain endothelial functions and opens the blood-brain/blood-glioma barrier; Med, Oncol. 21 21
-20°C
PATHWAY: Estrogen -- RESEARCH AREA: Neuroscience -- DISEASE AREA: Cancer