EGFR-IN-49

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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-49 

EGFR-IN-49 是一种有效的选择性 EGFR 抑制剂，对 EGFRT790M 和 EGFRT790M/L858R 的IC50 值分别为 65.0 nM 和 13.6 nM。EGFR-IN-49 以剂量依赖性方式诱导细胞凋亡 (apoptosis)。

EGFR-IN-49

EGFR-IN-49 Chemical Structure

CAS No. : 2459932-81-9

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生物活性

EGFR-IN-49 is a potent and selective EGFR inhibitor with IC50s of 65.0 nM and 13.6 nM for EGFRT790M and EGFRT790M/L858R, respectively. EGFR-IN-49 induces cell apoptosis in a dose-dependent manner[1].

IC50 & Target[1]

EGFRT790M

65.0 nM (IC50)

EGFRL858R/T790M

13.6 nM (IC50)

体外研究
(In Vitro)

EGFR-IN-49 (compound 13a) (1, 10 µM) shows inhibition activity for H1975 cells with an IC50 of 699.2 nM[1].
EGFR-IN-49 (1 µM) shows an strong inhibitory activity to EGFRT790M, EGFRT790M/L858R, EGFRWT with IC50s of 65.0, 13.6, >1000 nM, respectively[1].
EGFR-IN-49 (0.2, 4, 8 µM; 48 h) induces cell apoptosis in a dose-dependent manner in A431 cells[1].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: A549, A431, Hela, MCF7, LO2 cells
Concentration: 0-50 µM
Incubation Time:
Result: Showed excellent anti-proliferative activities with IC50s of 4.34, 3.79, 6.39, 18.99, >50 µM for A549, A431, Hela, MCF7, LO2 cells, respectively.

Apoptosis Analysis[1]

Cell Line: A431 cells
Concentration: 0.2, 4, 8 µM
Incubation Time: 48 h
Result: Induced cell apoptosis in a low concentration (0.33 µM) and exhibited higher percent of 16.41% % in the stage of late apoptotic at concentration of 4 µM.

分子量

413.45

Formula

C22H15N5O2S
CAS 号

2459932-81-9
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]. Xiao Z, et al. Design, synthesis and antitumor activity of novel thiophene-pyrimidine derivatives as EGFR inhibitors overcoming T790M and L858R/T790M mutations. Eur J Med Chem. 2020 Oct 1;203:112511.

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