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Ralaniten triacetate

Catalog No. T36375   CAS 1637573-04-6

Ralaniten triacetate (EPI-506) is a novel pro-drug of Ralaniten, functioning as an orally active inhibitor of the androgen receptor (AR) N-terminal domain (NTD). Its remarkable first-in-class status signifies its unique nature within the field. This compound exhibits significant efficacy against various AR species, including AR-v7, which are associated with resistance. Notably, Ralaniten triacetate's activity encompasses full-length AR as well [1][2].

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Ralaniten triacetate Chemical Structure
Ralaniten triacetate, CAS 1637573-04-6
Pack Size Availability Price/USD Quantity
1 mg In stock $ 165.00
5 mg In stock $ 413.00
10 mg In stock $ 689.00
25 mg In stock $ 1,490.00
50 mg In stock $ 1,980.00
100 mg In stock $ 2,500.00
1 mL * 10 mM (in DMSO) In stock $ 473.00
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Purity: 99.37%
ee: 97.98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Ralaniten triacetate (EPI-506) is a novel pro-drug of Ralaniten, functioning as an orally active inhibitor of the androgen receptor (AR) N-terminal domain (NTD). Its remarkable first-in-class status signifies its unique nature within the field. This compound exhibits significant efficacy against various AR species, including AR-v7, which are associated with resistance. Notably, Ralaniten triacetate's activity encompasses full-length AR as well [1][2].
In vitro Ralaniten triacetate (EPI-506) is designed to specifically target the N-terminal domain (NTD) of the androgen receptor (AR), serving as a pioneering treatment option in metastatic castration-resistant prostate cancer (mCRPC) research. As a first-of-its-kind, highly specific small molecule, EPI-506 operates by directly inhibiting AR transcriptional activity. It achieves this through binding to the AR's novel target site, the NTD, thereby preventing the AR's interaction with transcriptional proteins[2].
Molecular Weight 521
Formula C27H33ClO8
CAS No. 1637573-04-6

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 100 mg/mL (191.94 mM), Sonication is recommended.

TargetMolReferences and Literature

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.

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Keywords

Ralaniten triacetate 1637573-04-6 Ralaniten Triacetate Ralaniten inhibitor inhibit

 

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