Acetic acid, 2-bromo-, (6S,8aR,8bR,10aR,11R,13aR)-11-[(1R)-1,5-dimethylhexyl]-2,3,5,6,7,8,8a,8b,10,10a,11,12,13,13a-tetradecahydro-2,8a,10a-trimethyl-1,3-dioxo-4a,13b-etheno-1H,9H-benzo[c]cyclopenta[h][1,2,4]triazolo[1,2-a]cinnolin-6-yl ester

Description

MeTC7 is a vitamin D receptor antagonist (IC₅₀ = 2.9 μM in a fluorescence polarization assay).¹ It inhibits vitamin D receptor transactivation in HEK293 cells (IC₅₀ = 20.8 μM). It decreases the viability of OVCAR-8, OV-2008, SKOV3, Caov-3, and IGROV-1 ovarian cancer cells in a concentration-dependent manner. MeTC7 (250 nM) reduces retinoid X receptor α (RXRα) and importin-4 protein levels in OV-2008 cells. It reduces tumor growth in an SH-SY5Y neuroblastoma mouse xenograft model when administered at a dose of 10 mg/kg.

References

1. Khazan, N., Kim, K.K., Hansen, J.N., et al. Identification of a vitamin-D receptor antagonist, MeTC7, which inhibits the growth of xenograft and transgenic tumors in vivo J. Med. Chem. 65(8),6039-6055(2022).