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PROTAC BET degrader-2

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Chemical Structure| 2093388-33-9 同义名 : -
CAS号 : 2093388-33-9
货号 : A1148016
分子式 : C41H42N10O6
纯度 : 98%
分子量 : 770.836
MDL号 : N/A
存储条件：

粉末

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 50 mg/mL(64.86 mM)，配合低频超声助溶，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-25 is PROTAC targeting on BET proteins, consist of a BET inhibitor HJB97 as the warhead ligand and a Lenalidomide analogue as the CRBN ligand. PROTAC BET degrader-25 at concentration of 10, 30 and 100nM 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 9.6nM and 72.3nM, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.30mL

0.26mL

0.13mL

6.49mL

1.30mL

0.65mL

12.97mL

2.59mL

1.30mL
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.