Gefitinib-based PROTAC 3

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Chemical Structure| 2230821-27-7 同义名 : Gefitinib-based Proteolysis-targeting Chimera 3
CAS号 : 2230821-27-7
货号 : A346407
分子式 : C47H57ClFN7O8S
纯度 : 99%+
分子量 : 934.51
MDL号 : MFCD32062811
存储条件：

Pure form Keep in dark place, inert atmosphere, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 60 mg/mL(64.2 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
生物活性
靶点

  • EGFR/ErbB1

    EGFR, DC50:22.3 nM
描述 Gefitinib-based PROTAC 3, which links an EGFR binding component to a von Hippel-Lindau ligand via a connector, triggers EGFR breakdown with DC50 values of 11.7 nM in HCC827 (exon 19 deletion) and 22.3 nM in H3255 (L858R mutation) cells, respectively[1].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

1.07mL

0.21mL

0.11mL

5.35mL

1.07mL

0.54mL

10.70mL

2.14mL

1.07mL
参考文献

[1]Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan 18;25(1):67-77.e3.