货号	规格	价格	上海	北京	珠海	重庆	武汉
S88607-1mg	≥96%	￥90.00 S88607-1mg ￥90.00 现货	5 5	-	-	-	-
S88607-5mg	≥96%	￥210.00 S88607-5mg ￥210.00 现货	4 4	-	-	-	-
S88607-10mg	≥96%	￥320.00 S88607-10mg ￥320.00 现货	5 5	-	-	-	-
S88607-25mg	≥96%	￥630.00 S88607-25mg ￥630.00 现货	6 6	-	-	-	-
S88607-50mg	≥96%	￥1080.00 S88607-50mg ￥1080.00 2-3天	0 货期：2-3天	-	-	-	-
S88607-100mg	≥96%	￥1830.00 S88607-100mg ￥1830.00 2-3天	0 货期：2-3天	-	-	-	-

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产品描述：

Gefitinib-based PROTAC 3, conjugating an EGFR binding element to a von Hippel-Lindau 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

靶点：

EGFR:11.7 nM (DC50, HCC827(exon 19 del) cells);EGFR:22.3 nM (DC50, H3255 (L858R mutantion) cells);PROTAC;EGFR

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 Analysis Cell Line: HCC827 cells expressing exon 19 del EGFR; H3255 cells expressing L858R EGFR Concentration: 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 cells Incubation Time: 24 hours Result: Degradation of both exon-19 deletion EGFR as well as the mutant isoform containing the L858R activating point mutation.

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.

溶解性：

Soluble in DMSO

保存条件：

2-8°C

配置溶液浓度参考：

	1mg	5mg	10mg
1 mM	1.07 ml	5.35 ml	10.701 ml
5 mM	0.214 ml	1.07 ml	2.14 ml
10 mM	0.107 ml	0.535 ml	1.07 ml
50 mM	0.021 ml	0.107 ml	0.214 ml

注意：

部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。

参考文献

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