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产品介绍
产品介绍
产品信息
简单描述
Gefitinib-based PROTAC 3 is a proteolysis-targeting chimera (PROTAC) comprised of the EGF receptor (EGFR) inhibitor gefitinib (Item No. 13166) linked to the von Hippel-Lindau (VHL) E3 ubiquitin ligase ligand VHL ligand 1 (Item No. 21591).1 In cell-based assays, gefitinib-based PROTAC 3 induces degradation of EGFR containing the activating mutation L858R or an exon 19 deletion with half-maximal degradation (DC50) values of 22.3 and 11.7 nM, respectively, but does not induce degradation of wild-type EGFR at concentrations up to 10 μM.WARNING This product is not for human or veterinary use.
商品描述
A PROTAC that drives mutant EGFR degradation
分子量
934.5
纯度
≥98%
产品类型
Biochemicals/PROTACs
背景
别名
Formal_Name:(2S,4R)-1-((S)-2-(3-(2-((5-((4-((3-chloro-4-fluorophenyl)amino)-7-methoxyquinazolin-6-yl)oxy)pentyl)oxy)ethoxy)propanamido)-3,3-dimethylbutanoyl)-4-hydroxy-N-(4-(4-methylthiazol-5-yl)benzyl)pyrrolidine-2-carboxamide;Synonyms:Gefitinib-based Proteolysis-targeting Chimera 3
研究领域
Cancer/Cell Signaling/Growth Factor Receptor Signaling,Cell Biology/Cell Signaling/Growth Factor Receptors/Proteolysis/Ubiquitin/Proteasome System
结构式
ClC1=CC(NC2=NC=NC3=C2C=C(OCCCCCOCCOCCC(N[C@@H](C(C)(C)C)C(N4C[C@H](O)C[C@H]4C(NCC5=CC=C(C6=C(C)N=CS6
分子式
C47H57ClFN7O8S
CAS号
2230821-27-7
制备和贮存
保存
≥ 4 years
溶解方法
DMF: 25 mg/ml
DMF:PBS (pH 7.2) (1:3): 0.25 mg/ml
DMSO: 16 mg/ml
Ethanol: 10 mg/ml
保存方式
-20°C
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