For research use only. Not for therapeutic Use.
Ralaniten triacetate (EPI-506), the pro-agent of Ralaniten, is a first-in-class, orally active androgen receptor (AR) N-terminal domain (NTD) inhibitor. Ralaniten triacetate shows activity against both full length and resistance-related AR species, including AR-v7[1][2].
Ralaniten triacetate (EPI-506) targets the N-terminal domain of the androgen receptor (AR), and is used for metastatic castration-resistant prostate cancer (mCRPC) research. EPI-506 is a first-in-class, highly-specific small molecule that binds to a novel target on the AR, the N-terminal domain (NTD) and directly inhibits AR transcriptional activity by blocking the interaction of the AR with transcriptional proteins[2].
| Catalog Number | I014809 |
| CAS Number | 1637573-04-6 |
| Synonyms | [(2S)-2-acetyloxy-3-[4-[2-[4-[(2S)-2-acetyloxy-3-chloropropoxy]phenyl]propan-2-yl]phenoxy]propyl] acetate |
| Molecular Formula | C27H33ClO8 |
| Purity | ≥95% |
| InChI | InChI=1S/C27H33ClO8/c1-18(29)32-16-26(36-20(3)31)17-34-24-12-8-22(9-13-24)27(4,5)21-6-10-23(11-7-21)33-15-25(14-28)35-19(2)30/h6-13,25-26H,14-17H2,1-5H3/t25-,26-/m1/s1 |
| InChIKey | HGHVYYKTOXUQNT-CLJLJLNGSA-N |
| SMILES | CC(=O)OCC(COC1=CC=C(C=C1)C(C)(C)C2=CC=C(C=C2)OCC(CCl)OC(=O)C)OC(=O)C |
| Reference | [1]. Obst JK, et al. Revealing Metabolic Liabilities of Ralaniten To Enhance Novel Androgen Receptor Targeted Therapies. ACS Pharmacol Transl Sci. 2019;2(6):453-467. Published 2019 Sep 26. [2]. Chi, Kim Nguyen et al. Efficacy, safety, tolerability, and pharmacokinetics of EPI-506 (ralaniten acetate), a novel androgen receptor (AR) N-terminal domain (NTD) inhibitor, in men with metastatic castration-resistant prostate cancer (mCRPC) progressing after enzalutamide and/or abiraterone. Journal of Clinical Oncology 35 (2017): 5032-5032. |
