1. JAK/STAT Signaling Protein Tyrosine Kinase/RTK
  2. EGFR
  3. EGFR-IN-49

EGFR-IN-49 是一种有效的选择性 EGFR 抑制剂,对 EGFRT790MEGFRT790M/L858RIC50 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晚期凋亡 (apoptosis)。

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EGFR-IN-49 Chemical Structure

EGFR-IN-49 Chemical Structure

CAS No. : 2459932-81-9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

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 late 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].

MCE 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
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.

纯度 & 产品资料
参考文献
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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EGFR-IN-49
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HY-146782
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