Chemical Structure : UNC8732 TFA
CAS No.:
2929304-06-1
UNC8732 TFA
(UNC 8732 TFA)
Catalog No.: PC-22589Not For Human Use, Lab Use Only.
UNC8732 TFA is a highly potent, second-generation NSD2 degrader with DC50 of 0.06 uM and Dmax of 97%, SPR KD of 76 nM, facilitates FBXO22-mediated degradation of NSD2 in NSD2-mutant ALL.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
UNC8732 TFA is a highly potent, second-generation NSD2 degrader with DC50 of 0.06 uM and Dmax of 97%, SPR KD of 76 nM, facilitates FBXO22-mediated degradation of NSD2 in NSD2-mutant ALL.
UNC8732 demonstrates improved NSD2 degradation and H3K36me2 reduction in cells, compared with UNC8153.
UNC8732 promotes highly selective NSD2 degradation within the measurable proteome.
UNC8732 inhibits cell growth and restores GC sensitivity of NSD2 p.E1099K mutant ALL cells, induces apoptosis of NSD2 mutant cells.
The metabolism of UNC8732 to the aldehyde is required for effective degradation.
UNC8732 recruits the SCFFBXO22 ubiquitin ligase complex for compound-mediated degradation of NSD2, binds and recruits FBXO22 via interactions with C326.
Physicochemical Properties
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M.Wt
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723.75
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Formula
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C37H40F3N5O7
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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-(4-((2-(6-aminohexanoyl)-1,2,3,4-tetrahydroisoquinolin-6-yl)carbamoyl)benzyl)-N-cyclopropyl-3-oxo-3,4-dihydro-2H-benzo[b][1,4]oxazine-7-carboxamide 2,2,2-trifluoroacetate
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References
1. Nie DY, et al. Nat Chem Biol. 2024 Jul 4. doi: 10.1038/s41589-024-01660-y.
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