1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEGefitinib-based PROTAC 3Cat. No.: HY-123921CAS No.: 2230821-27-7分式: CHClFNOS分量: 934.51作靶點: EGFR; PROTAC作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK; PROTAC儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1

2、month溶解性數(shù)據(jù)體外實驗 DMSO : 60 mg/mL (64.20 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.0701 mL 5.3504 mL 10.7008 mL5 mM 0.2140 mL 1.0701 mL 2.1402 mL10 mM 0.1070 mL 0.5350 mL 1.0701 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙?/p>

3、案，配制前請先配制澄清的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1 mg/mL (1.07 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1 mg/mL (1.07 mM); Clear solution1/2 Master of Sm

4、all Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 Gefitinib-based PROTAC 3，通過 linker 將 EGFR 結(jié)合元件與 VHL 配體結(jié)合，作于 HCC827 (外顯 19 缺失)和 H3255 (L858R 突變) 細(xì)胞，誘導(dǎo) EGFR 降解，DC50 分別為 11.7 nM 和 22.3 nM 1。IC50 & Target EGFR EGFR PROTAC11.7 nM (DC50, HCC827(exon 19 22.3 nM (DC50, H3255 (L858Rdel) cells) mutant

5、ion) cells)體外研究 H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 M; 24 hours),HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 M; 24hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isof

6、ormcontaining the L858R activating point mutation, while sparing the WT EGFR 1.Western Blot Analysis 1Cell Line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFRConcentration: 100 nM, 250 nM, 1 M, 2.5 M, 10 M for HCC827 cells; 25 nM, 100 nM, 1 M, 2.5 M,10 M for H3255 cells

7、Incubation Time: 24 hoursResult: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing theL858R activating point mutation.REFERENCES1. Burslem GM, et al. The Advantages of Targeted Protein Degradation Over Inhibition: An RTK Case Study. Cell Chem Biol. 2018 Jan18;25(1):67-77.e3.McePdfHeightCaution: Product has not been fully validated for medical applications.For research