Biological descriptionCompetitive estrogen receptor antagonist and partial agonist. Inhibits estrogen dependent gene transcription and tumor growth. Additionally decreases cardiac infarction and inhibits Kir2.1, Kir2.2 and Kir2.3 potassium channels (IC50 values are 0.93, 0.87 and 0.31 µM, respectively).
Chemical name(Z)-2-[4-(1,2-Diphenyl-1-butenyl)phenoxy]-N,N-dimethylethanamine citrate
Storage instructionsStore at +4°C. The product can be stored for up to 12 months.
Solubility overviewSoluble in DMSO to 100 mM and in ethanol to 5 mM
Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.
Ponce-Balbuena D et al. Tamoxifen inhibits inward rectifier K+ 2.x family of inward rectifier channels by interfering with phosphatidylinositol 4,5-bisphosphate-channel interactions. J Pharmacol Exp Ther331:563-73 (2009).
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Massarweh S et al. Tamoxifen resistance in breast tumors is driven by growth factor receptor signaling with repression of classic estrogen receptor genomic function. Cancer Res68:826-33 (2008).
Read more (PubMed: 18245484) »