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首页-抗体药物偶连体和PROTACs-PROTAC-ITRI-148
ITRI-148

Chemical Structure : ITRI-148

CAS No.:

ITRI-148

货号: PC-26228Not For Human Use, Lab Use Only.

ITRI-148 is a CRBN-based androgen receptor N-terminal domain (AR-NTD) degrader, degrades AR, AR-V7, and AR mutants with DC50 of 0.05 uM and 0.02 uM for AR and AR-V7in VCaP cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ITRI-148 is a CRBN-based androgen receptor N-terminal domain (AR-NTD) degrader, degrades AR, AR-V7, and AR mutants with DC50 of 0.05 uM and 0.02 uM for AR and AR-V7in VCaP cells.
ITRI-148 degrades AR and AR-V7 via the proteasome-dependent system。
ITRI-148 specifically targets the AR pathway.
ITRI-148 potently inhibits the viability of CRPC and enzalutamide-resistant cells.
ITRI-148 is orally bioavailable and exhibits potent antitumor activity in SCID mice bearing VCaP xenografts.

物理化学性质&存储条件

分子量 851.94
分子式 C44H48F3N11O4
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

2-(6-imino-2-oxopiperidin-3-yl)-4-((2-oxo-2-(4-((4-(1-(3-(trifluoromethyl)-7,8-dihydro-[1,2,4]triazolo[4,3-b]pyridazin-6-yl)piperidin-4-yl)phenyl)ethynyl)-[1,4'-bipiperidin]-1'-yl)ethyl)amino)isoindoline-1,3-dione

参考文献

1. Chiu-Lien Hung, et al. Neoplasia. 2026 Jan:71:101253. doi: 10.1016/j.neo.2025.101253.

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