Here, we show that the VDR antagonist MeTC7 (5), which can be synthesized from 7-dehydrocholesterol (6) in two steps, inhibits VDR selectively, suppresses theviability of cancer cell-lines, and reduces the growth of the spontaneoustransgenic TH-MYCN neuroblastoma and xenografts in vivo. Here, VDR is linked to cancer.