Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate made of Melatonin and Tamoxifen, serving as an effective antagonist of ERalpha (IC50 = 863 nM). In cells expressing the hMT1 receptor, it binds to MLT receptors (Ki = 3.1 nM) and exhibits the ability to promote beta-arrestin activation (EC50 = 914 nM) and ERK activation (EC50 = 98 nM). The IC50 values for Melatonin-Tamoxifen Conjugate in MCF-7, MDA-MB-231, and HT-1080 cell lines are 6.8 µM, 6.4 µM, and 1.7 µM, respectively.
Molekulargewicht:
742.99
Formel:
C47H58N4O4
Target-Kategorie:
Melatonin Receptor
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