2230821-27-7|Gefitinib-based PROTAC 3|CsnPharm

CAS No.: 2230821-27-7

Gefitinib-based PROTAC 3 Catalog No. CSN22297

Synonyms: Gefitinib-based Proteolysis-targeting Chimera 3;NTN-21277

Gefitinib-based PROTAC 3 is a VHL-recruiting PROTAC that induces the degradation of EGFR and EGFR mutants with DC50 of 11.7 nM and 22.3 nM for HCC827 cell (Exon 19 del) and H3255 cell (L858R).

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400-920-2911

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技术信息

生物活性

描述Gefitinib-based PROTAC targeting on EGFR, consist of Gefitinib as the warhead linked to VHL-recruiting ligand, with DC₅₀ value/D_max value of 11.7nM/98.9% and 22.3nM/96.6% for degradation of EGFR in HCC827 cells expressing exon 19 del EGFR and H3255 cells expressing L858R EGFR, respectively, post 24-hour treatment.
参考文献

[1] Burslem GM, Smith BE, 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 1.0701 mL
- 5.3504 mL
- 10.7008 mL
- 5 mM
- 0.2140 mL
- 1.0701 mL
- 2.1402 mL
- 10 mM
- 0.1070 mL
- 0.5350 mL
- 1.0701 mL

技术信息

CAS号

2230821-27-7

储存条件

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

液体: -20°C:3-6 月 -80°C:12月

分子式

C47H57ClFN7O8S

运输

蓝冰

分子量

934.51

别名

Gefitinib-based Proteolysis-targeting Chimera 3;NTN-21277

溶解度

DMSO	75.0 mg/mL (80.3 mM)
Water	insoluble

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Gefitinib-based PROTAC 3 Catalog No. CSN22297

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