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Gefitinib-based PROTAC 3
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Gefitinib-based PROTAC 3图片
CAS NO:2230821-27-7
包装与价格:
包装价格(元)
1 mg电议
2 mg电议
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
500 mg电议

产品介绍
Gefitinib-based PROTAC 3 通过 linker 将EGFR结合元件与von Hippel-Lindau配体结合,在 HCC827(外显子 19 del)和 H3255(L858R 突变)细胞中诱导 EGFR 降解,DC50 分别为 11.7 和 22.3 nM。

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].

体外活性

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].

Cas No.

2230821-27-7

分子式

C47H57ClFN7O8S

分子量

934.52

储存和溶解度

DMSO:10 mM
Powder: -20°C for 3 years
In solvent: -80°C for 2 years