1817841-22-7

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.

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).