| Identification | Back Directory | [Name]
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 | [CAS]
1817841-22-7 | [Synonyms]
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 | [Molecular Formula]
C32H48BrN3O4 | [MOL File]
1817841-22-7.mol | [Molecular Weight]
618.66 |
| Chemical Properties | Back Directory | [Boiling point ]
619.5±65.0 °C(Predicted) | [density ]
1.32±0.1 g/cm3(Predicted) | [solubility ]
Ethanol: 1 mg/ml | [form ]
A crystalline solid | [pka]
-2.59±0.70(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [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. | [Uses]
MeTC7 is a Vitamin-D receptor (VDR) antagonist. MeTC7 has potent VDR inhibition activity with an IC50 value of 2.9 μM. MeTC7 shows good antitumor effects[1]. | [in vivo]
MeTC7 (compound 5) (i.p.; 10 mg/kg) reduces the growth of the spontaneous transgenic TH-MYCN neuroblastoma and xenografts in vivo[1]. | Animal Model: | Mice[1] | | Dosage: | 10 mg/kg | | Administration: | IP | | Result: | Reduced the growth of xenografts derived from ovarian cancer, medulloblastoma, and pancreatic cancer cells.
Inhibited the growth of neuroblastoma cells and Xenografts.
Reduced MYCN expression and blocked the growth of TH-MYCN transgene-driven spontaneous neuroblastoma.
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| [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). |
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