Chemical Structure : TRIB2 PROTAC 5k
CAS No.:
TRIB2 PROTAC 5k
(Compound 5k)
Catalog No.: PC-23445Not For Human Use, Lab Use Only.
TRIB2 PROTAC 5k (Compound 5k) is a potent, selective pseudokinase TRIB2 PROTAC degrader with DC50 of 16.8 nM and Dmax of 92% in PC3 cells.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
TRIB2 PROTAC 5k (Compound 5k) is a potent, selective pseudokinase TRIB2 PROTAC degrader with DC50 of 16.8 nM and Dmax of 92% in PC3 cells.
Compound 5k also demonstrates potent degradation activity against TRIB2 protein levels in other prostate cancer cell lines including H660 and LTL-331R-CL neuroendocrine prostate cancer cells.
Compound 5k facilitates TRIB2 degradation via Cereblon-dependent ubiquitination and proteasomal pathways.
Compound 5k dose-dependently inhibits the ATP binding affinity of TRIB2 with IC50 of 65.2 nM.
Compound 5k exhibits selectivity towards TRIB2 over other pseudokinases.
Compound 5k shows potent anti-proliferative and apoptotic effects in AR- prostate cancer cell lines (neuroendocrine-like LTL-331R-CL cells, IC50=3.9 nM, PC3 cell IC50=30.38 nM).
Compound 5k triggers apoptosis in a panel of prostate cancer cell lines (LTL-331R-CL and PC3 cells).
Physicochemical Properties
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M.Wt
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812.90
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Formula
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C45H45FN8O6
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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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N-(2-(10-((2-(2,6-dioxopiperidin-3-yl)-1,3-dioxoisoindolin-5-yl)amino)-decanoyl)-1,2,3,4-tetrahydroisoquinolin-7-yl)-5-(2-fluoropyridin-3-yl)-1H-indazole-3-carboxamide
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References
1. Wen C, et al. Eur J Med Chem. 2024 Nov 1;281:117016.
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