Bioactivity | Melatonin-Tamoxifen Conjugate (compound 16c) is an anticancer drug conjugate composed of Melatonin (HY-B0075) and Tamoxifen (HY-13757A), which is a potent antagonist of ERα (IC50=863 nM). Melatonin-Tamoxifen Conjugate binds to MLT receptor (Ki=3.1 nM) and promotes β-arrestin (EC50=914 nM) and ERK activation (EC50=98 nM) in cells expressing hMT1 receptor. Melatonin-Tamoxifen Conjugate against several common cell lines MCF-7, MDA-MB-231, and HT-1080 with IC50s of 6.8 μM, 6.4 μM, and 1.7 μM, respectively. |
Formula | C47H58N4O4 |
Molar Mass | 742.99 |
Transport | Room temperature in continental US; may vary elsewhere. |
Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
Reference | [1]. Marzouk MA, et al. Cancer Cells Show Higher Sensitivity to Melatonin-Tamoxifen Drug Conjugates than to Combination of Melatonin and Tamoxifen. ACS Omega. 2024 Nov 18;9(48):47857-47871. |