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PROTAC B-Raf degrader 1

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Chemical Structure| 2364367-27-9 同义名 : -
CAS号 : 2364367-27-9
货号 : A1148709
分子式 : C36H37N5O12S
纯度 : 98%
分子量 : 763.77
MDL号 : N/A
存储条件：

粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 25 mg/mL(32.73 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 B-Raf degrader 2 is a PROTAC targeting on B-Raf, consist of B-Raf ligand RGS linked to CRBN ligand Pomalidomide. PROTAC B-Raf degrader 2 led to a significant degradation of B-Raf at concentration of both 5μM and 10μM in MCF-7 cells post 24h, accompanied with a downregulation of its downstream Mcl-1. PROTAC B-Raf degrader 2 at concentration of 20μM achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) and arrested cell cycle at the same G2/M phase in MCF-7 cells post 24h. PROTAC B-Raf degrader 2 exhibited cytotoxicity to MCF-7, MDA-MB-231, HepG2, LO2 and B16 cell lines with IC50 values of 2.70, 21.21, 18.70, 41.11 and 22.68μM, respectively, post 72-hour treatment[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.31mL

0.26mL

0.13mL

6.55mL

1.31mL

0.65mL

13.09mL

2.62mL

1.31mL
参考文献

[1]Chen H, Chen F, et al. Pomalidomide hybrids act as proteolysis targeting chimeras: Synthesis, anticancer activity and B-Raf degradation. Bioorg Chem. 2019 Jun;87:191-199.