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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-EPI-7386
EPI-7386

Chemical Structure : EPI-7386

CAS No.: 2416716-62-4

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EPI-7386 (Masofaniten)

货号: PC-22814Not For Human Use, Lab Use Only.

EPI-7386 (Masofaniten) is a next-generation androgen receptor N-terminal domain (AR NTD) inhibitor, inhibits AR activity by binding the N-terminal domain (NTD) and blocking transcription, irrespective of ligand-binding domain resistance mechanisms.

规格 价格 库存 数量
5 mg ￥3580 In stock
10 mg ￥5580 In stock
25 mg ￥9580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

EPI-7386 (Masofaniten) is a next-generation androgen receptor N-terminal domain (AR NTD) inhibitor, inhibits AR activity by binding the N-terminal domain (NTD) and blocking transcription, irrespective of ligand-binding domain resistance mechanisms.
EPI-7386 exhibited potent activity in inhibiting full-length AR (AR-FL) driven transcriptional activity and also strongly impaired the transcriptional activity and the viability of cellular models driven exclusively by truncated AR protein.
EPI-7386 inhibits androgen-activated AR binding to target gene loci such as KLK3.
EPI-7386 suppresses AR-regulated target gene expression in a comparable manner as lutamides in three human prostate cancer cell lines, LNCaP, 22Rv1, and VCaP.
The combination of EPI-7386 with lutamides resulted in broader and deeper inhibition of AR-associated transcriptional activity in both LNCaP and VCaP cells.

物理化学性质&存储条件

分子量 535.44
分子式 C24H24Cl2N4O4S
外观性状 Solid
CAS No.
储存条件
固体粉末
-20°C 12 个月; 4°C 6 个月
配置液
-80°C 6 个月; -20°C 6 个月
Shipping
Solubility

10 mM in DMSO
Chemical Name/SMILES

Methanesulfonamide, N-[4-[[4-[1-[3-chloro-4-(2-chloroethoxy)-5-cyanophenyl]-1-methylethyl]phenoxy]methyl]-2-pyrimidinyl]-

参考文献

1. Obst JK, et al. Steroids. 2024 Jul 23;210:109482.

2. Nan Hyung Hong, et al. Cancer Res (2021) 81 (13_Supplement): 1209.

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