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首页-抗体药物偶连体和PROTACs-PROTAC-UNC8732 TFA
UNC8732 TFA

Chemical Structure : UNC8732 TFA

CAS No.: 2929304-06-1

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UNC8732 TFA (UNC 8732 TFA)

货号: 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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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

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.

物理化学性质&存储条件

分子量 723.75
分子式 C37H40F3N5O7
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-(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

参考文献

1. Nie DY, et al. Nat Chem Biol. 2024 Jul 4. doi: 10.1038/s41589-024-01660-y.

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