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首页-抗体药物偶连体和PROTACs-PROTAC-dBET1
dBET1

Chemical Structure : dBET1

CAS No.: 1799711-21-9

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dBET1 (dBET 1)

货号: PC-62321Not For Human Use, Lab Use Only.

dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex.

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

生物&药学活性

dBET1 is a proteolysis-targeting chimera (PROTAC) molecule that appendes a competitive antagonist of BET bromodomain (JQ1) to a phthalimide moiety to hijack the cereblon E3 ubiquitin ligase complex.
dBET1 induces highly selective cereblon-dependent BET protein degradation in vitro (EC50=430 nM) and in vivo and delayed leukemia progression in mice.

物理化学性质&存储条件

分子量 785.273
分子式 C38H37ClN8O7S
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

(6S)-4-(4-chlorophenyl)-N-[4-[[2-[[2-(2,6-dioxo-3-piperidinyl)-2,3-dihydro-1,3-dioxo-1H-isoindol-4-yl]oxy]acetyl]amino]butyl]-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

参考文献

1. Winter GE, et al. Science. 2015 Jun 19;348(6241):1376-81.

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