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抑制剂描述:

产品名称:Gefitinib-based PROTAC 3

产品别名:见爱必信官网

英文别名:Gefitinib-based PROTAC 3

靶点:

CAS:2230821-27-7

纯度:98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a VHL ligand via a linker, induces EGFR degradation with DC50s of 11.7 nM and 22.3 nM in HCC827(exon 19 del) and H3255 (L858R mutantion) cells, respectively.

溶解性:Soluble in DMSO

体外研究:

H3255 cells expressing L858R EGFR treated with Gefitinib-based PROTAC 3 (25 nM-10 μM; 24 hours), HCC827 cells expressing exon 19 del EGFR treated with Gefitinib-based PROTAC 3 (100 nM-10 μM; 24 hours), which enables the degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation, while sparing the WT EGFR.Western Blot AnalysisCell Line:HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFRConcentration:100 nM, 250 nM, 1 μM, 2.5 μM, 10 μM for HCC827 cells; 25 nM, 100 nM, 1 μM, 2.5 μM, 10 μM for H3255 cellsIncubation Time:24 hoursResult:Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.

体内研究:

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