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PROTAC BET Degrader 9

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Chemical Structure| 2093386-22-0 同义名 : PROTAC BET Degrader-1
CAS号 : 2093386-22-0
货号 : A482817
分子式 : C44H45N11O9
纯度 : 98%
分子量 : 871.896
MDL号 : MFCD31692340
存储条件:

粉末 Keep in dark place,Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月

溶解度 :

DMSO: 50 mg/mL(57.35 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO

动物实验配方:
生物活性
描述 PROTAC BET degrader-9 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and Pomalidomide as CRBN ligand. PROTAC BET degrader-9 at concentration of 3, 10 and 30nM led a dose-dependent degradation of BRD2, 3 and 4 at different levels post 3-hour treatment in RS4;11 cells. PROTAC BET degrader-25 exhibited potency against MOLM-13 and RS4;11 with IC50 values of 4.3nM and 45.5nM, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.15mL

0.23mL

0.11mL

5.73mL

1.15mL

0.57mL

11.47mL

2.29mL

1.15mL

参考文献

[1]Zhou B, Hu J, et al. Discovery of a Small-Molecule Degrader of Bromodomain and Extra-Terminal (BET) Proteins with Picomolar Cellular Potencies and Capable of Achieving Tumor Regression. J Med Chem. 2018 Jan 25;61(2):462-481.