EGFR-IN-46

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

EGFR-IN-46 

EGFR-IN-46 是一种有效的 EGFR 和 FAK 双重抑制剂，IC50s 分别为 20.17 nM，14.25 nM。EGFR-IN-46 显著抑制癌细胞的生长。EGFR-IN-46 诱导细胞凋亡 (apoptosis)sup>[1]。

EGFR-IN-46

EGFR-IN-46 Chemical Structure

CAS No. : 2764772-88-3

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生物活性

EGFR-IN-46 is a potent EGFR and FAK dual inhibitor with IC50s of 20.17 nM, 14.25 nM, respectively. EGFR-IN-46 significantly inhibits the growth of cancer cells. EGFR-IN-46 induces cell apoptosis[1].

IC50 & Target[1]

EGFR

20.17 nM (IC50)

FAK

14.25 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-46 (compound 6h) (0-100 µM; 24 h) inhibits the growth activity against DLD1, HCT-116 cells with IC50s of 1.79, 3.28 µM, respectively[1].
EGFR-IN-46 (3 µM; 24 h) induces cell apoptosis in DLD1 cells[1].
EGFR-IN-46 exhibits weak TOP1 (Topoisomerase I) poisoning effect (-/+)[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: DLD1, HCT-116, MDMBA-231, MCF-7, Hela cells
Concentration: 10 µM
Incubation Time: 24 h
Result: Showed excellent growth inhibition with the percent growth inhibition of 92.36%, 89.34%, 84.76%, 90.36%, 90.78% for DLD1, HCT-116, MDMBA-231, MCF-7, Hela cells, respectively.

Apoptosis Analysis[1]

Cell Line: DLD1 cells
Concentration: 3 µM
Incubation Time: 24 h
Result: Increased the total percentage of apoptotic cells from 7% to 90.33%.

分子量

503.56

Formula

C27H32F3N3O3
CAS 号

2764772-88-3
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
参考文献

  • [1]. Elbadawi MM, et al. 2-Arylquinolines as novel anticancer agents with dual EGFR/FAK kinase inhibitory activity: synthesis, biological evaluation, and molecular modelling insights. J Enzyme Inhib Med Chem. 2022 Dec;37(1):349-372.

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