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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Androgen Receptor (AR)-ET516
ET516

Chemical Structure : ET516

CAS No.: 2820120-95-2

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ET516 (ET-516)

货号: PC-20115Not For Human Use, Lab Use Only.

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

ET516 is a potent androgen receptor liquid-liquid phase separation (AR LLPS) inhibitor, specifically disrupts AR condensates, effectively suppresses AR transcriptional activity and inhibits the proliferation and tumor growth of prostate cancer cells expressing AR-resistant mutants.
ET516 dose-dependently inhibited the ARE reporter activity and condensate formation of AR(F877L/T878A) with IC50 of 0.7 μM and 0.2 μM, respectively.
ET516 potently inhibited the phase separation capability and transcriptional activation of AR(WT), AR(T878A) and AR(W742C) without inducing nuclear translocation of AR or affecting AR protein levels.
ET516, but not enzalutamide, also suppressed the puncta formation and transcriptional activity of constitutively active AR splice variant AR(V7).
ET516 (10 uM) specifically reduced AR transcriptional activity and inhibits growth of CRPC, reduced the proliferation of AR-positive LNCaP and VCaP cells, but not that of AR-negative PC3 cells.
ET516 efficiently inhibited the growth of both enzalutamide-resistant mutants AR(F877L/T878A), and AR(V7) expressing cells, but not enzalutamide.
ET516 (30mg/kg, p.o., BID) reduced tumor growth of LNCaP-AR(F877L/T878A) xenografts.

物理化学性质&存储条件

分子量 529.44
分子式 C25H22Cl2N4O3S
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

N-(5-((4-(2-(3-chloro-4-(2-chloroethoxy)-5-cyanophenyl)propan-2-yl)phenyl)ethynyl)pyrimidin-2-yl)methanesulfonamide

参考文献

1. Jingjing Xie, et al. Nat Chem Biol. 2022 Dec;18(12):1341-1350.

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