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首页-抗体药物偶连体和PROTACs-PROTAC-UNC8153 TFA
UNC8153 TFA

Chemical Structure : UNC8153 TFA

CAS No.: 2929304-61-8

UNC8153 TFA (UNC 8153 TFA)

货号: PC-22591Not For Human Use, Lab Use Only.

UNC8153 (UNC 8153) TFA is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces the cellular levels of both NSD2 protein (DC50=350 nM) and the H3K36me2 chromatin mark.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

UNC8153 (UNC 8153) TFA is a selective NSD2-targeted degrader with binding Kd of 24 nM for NSD2, potently and selectively reduces the cellular levels of both NSD2 protein (DC50=350 nM) and the H3K36me2 chromatin mark.
UNC8153 contains a simple warhead that confers proteasome-dependent degradation of NSD2 through a novel mechanism.
UNC8153 downregulates pathological phenotypes in multiple myeloma cells including mild antiproliferative effects in MM1.S cells containing an activating point mutation and antiadhesive effects in KMS11 cells harboring the t(4;14) translocation.

物理化学性质&存储条件

分子量 697.71
分子式 C35H38F3N5O7
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-((4-((6-aminohexyl)carbamoyl)phenyl)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. Ronan P Hanley, et al. J Am Chem Soc. 2023 Mar 28. doi: 10.1021/jacs.3c01421.

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