Aromatase-IN-8 is a selective aromatase inhibitor with an IC50 of 0.05 µM for aromatase activity. It exhibits selective antiproliferative effects on estrogen receptor-positive breast cancer cell lines while being non-toxic to non-tumor cells. Aromatase-IN-8 suppresses estrogen activity, elevates testosterone levels, and downregulates estrogen receptor expression and phosphorylation. It is applicable for research in triple-negative breast cancer.

Aromatase:0.05 μM

Aromatase-IN-8 (compound 17) demonstrates significant anticancer activity in estrogen receptor-positive breast cancer cell lines (T47D and MCF-7) and triple-negative breast cancer cell lines (MDA-MB-231), with IC50 values of 42.90 µM, 79.43 µM, and >100 µM, respectively. In concentrations ranging from 6.25 to 100 µM over 24 and 72 hours, Aromatase-IN-8 shows a dose-dependent reduction in cell viability in MCF-7 and MDA-MB-231 cells. Additionally, 0-50 μM over 24 hours reduces ERα and ERβ protein levels in MCF-7 cells. At concentrations of 6.25-50 μM for 8 hours, it decreases 17β-estradiol and estrone levels, mildly inhibiting estrogen synthesis, while testosterone accumulation becomes more pronounced above 12.5 µM. Moreover, Aromatase-IN-8 downregulates fatty acid degradation, upregulates pantothenic acid and Coenzyme A biosynthesis, and promotes valine and sphinganine accumulation, exhibiting potent anticancer effects at higher doses in MCF-7 cells.