Gefitinib-based PROTAC 3CS-01Y78454_上海莼试生物技术有限公司

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一、概述：

化学性质：

规格	1mg 5mg 25mg
CAS	2230821-27-7
别名	N/A
化学名	N/A
分子式	C47H57ClFN7O8S
分子量	934.522
溶解度	DMF: 25 mg/ml,DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml,DMSO: 16 mg/ml,Ethanol: 10 mg/ml
储存条件	4°C, away from moisture and light
General tips	For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping Condition	Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request

产品描述：

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[1].

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[1].

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标签：Gefitinib-based PROTAC 3

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