Ralaniten triacetate

Modify Date: 2024-01-17 14:57:51

Ralaniten triacetate Structure
Ralaniten triacetate structure
Common Name Ralaniten triacetate
CAS Number 1637573-04-6 Molecular Weight 521.00
Density N/A Boiling Point N/A
Molecular Formula C27H33ClO8 Melting Point N/A
MSDS N/A Flash Point N/A

 Use of Ralaniten triacetate


Ralaniten triacetate (EPI-506), the pro-drug 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].

 Names

Name Ralaniten triacetate

 Ralaniten triacetate Biological Activity

Description Ralaniten triacetate (EPI-506), the pro-drug 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].
Related Catalog
In Vitro 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].
References

[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.

 Chemical & Physical Properties

Molecular Formula C27H33ClO8
Molecular Weight 521.00