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CRBN PROTAC compound I

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Chemical Structure| 2244520-98-5 同义名 : Homo-PROTAC cereblon degrader 1;OUN20985;Homo-PROTAC cereblon degrader 1, OUN20985
CAS号 : 2244520-98-5
货号 : A1147988
分子式 : C32H32N6O10
纯度 : 98%
分子量 : 660.631
MDL号 : MFCD31813818
存储条件：

粉末 Keep in dark place,Inert atmosphere,2-8°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 190 mg/mL(287.6 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
靶点

  • CRBN
描述 Homo-PROTAC cereblon degrader 15a is a PROTAC selectively targeting on CRBN, consist of two linked Pomalidomide as warhead and E3 ligase ligand. Homo-PROTAC cereblon degrader 15a led a dose-dependent degradation of CRBN at concentration ranging in 1-100nM post 16h, with almost no effect on IKZF1, in MM1S cells. Homo-PROTAC cereblon degrader 15a at concentration<1μM did not affect proliferation of different cell lines, including OCI-AML5, MM1S and NCI-H929 cells, due to the prevention of pomalidomide-induced degradation of IKZF1 and IKZF3. Also, it antagonized the effects of pomalidomide on multiple myeloma cells[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.51mL

0.30mL

0.15mL

7.57mL

1.51mL

0.76mL

15.14mL

3.03mL

1.51mL
参考文献

[1]Steinebach C, Lindner S, et al. Homo-PROTACs for the Chemical Knockdown of Cereblon. ACS Chem Biol. 2018 Sep 21;13(9):2771-2782.