Chemical Structure : ITRI-148
CAS No.:
ITRI-148
Catalog No.: 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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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
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.
Physicochemical Properties
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M.Wt
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851.94
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Formula
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C44H48F3N11O4
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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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
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References
1. Chiu-Lien Hung, et al. Neoplasia. 2026 Jan:71:101253. doi: 10.1016/j.neo.2025.101253.
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