| Identification | Back Directory | [Name]
Methanesulfonamide, N-[(2R)-3-[4-[1-[3,5-dichloro-4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]-1-methylethyl]phenoxy]-2-hydroxypropyl]- | [CAS]
2139288-26-7 | [Synonyms]
Methanesulfonamide, N-[(2R)-3-[4-[1-[3,5-dichloro-4-[(2S)-3-chloro-2-hydroxypropoxy]phenyl]-1-methylethyl]phenoxy]-2-hydroxypropyl]- | [Molecular Formula]
C22H28Cl3NO6S | [MOL File]
2139288-26-7.mol | [Molecular Weight]
540.88 |
| Chemical Properties | Back Directory | [Boiling point ]
694.7±65.0 °C(Predicted) | [density ]
1.372±0.06 g/cm3(Predicted) | [form ]
Solid | [pka]
10.36±0.40(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Description]
EPI-7170 is a potent androgen receptor N-terminal domain antagonist, decreasing expression of DNA repair genes, sensitizing prostate cancer cells that express full-length AR and AR-Vs to radiotherapy. | [Uses]
EPI-7170, a ralaniten analogue, is a potent androgen receptor N-terminal structural domain antagonist that blocks the transcriptional activity of full-length AR (FL-AR) and AR splice variants (AR-Vs). EPI-7170 has antitumor effects against enzalutamide resistant castration-resistant prostate cancer (CRPC)[1]. | [in vivo]
EPI-7170 (oral administration, 30 mg/kg, daily, 31 days) has some anti-tumor activity and can be combined with enzalutamide in male NOD/SCID mice[1].
| Animal Model: | 6-8 week old male NOD/SCID mice infected with VCaP-ENZR cells[1] | | Dosage: | 30 mg/kg | | Administration: | Oral administration; daily; 31 days | | Result: | Significantly reduced tumor volume and decreased levels of FL-AR and AR-V7 in harvested xenografts. |
| [References]
[1] Hirayama Y, et al. Combination therapy with androgen receptor N-terminal domain antagonist EPI-7170 and enzalutamide yields synergistic activity in AR-V7-positive prostate cancer. Mol Oncol. 2020 Oct;14(10):2455-2470. DOI:10.1002/1878-0261.12770 |
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