2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR Apoptosis Metabolic Enzyme/Protease Immunology/Inflammation NF-κB
  3. EGFR PI3K Akt Apoptosis Reactive Oxygen Species (ROS) Mitochondrial Metabolism
  4. EGFR-IN-196

EGFR-IN-196 是一种 EGFR 抑制剂，其 IC50 为 105.96 nM。EGFR-IN-196 可抑制 EGFR 的酶活性，降低磷酸化 PI3K 水平，并抑制下游 EGFR-AKT 信号通路。EGFR-IN-196 可增加细胞内活性氧 (ROS) 的生成，诱导线粒体去极化，并诱导癌细胞凋亡 (apoptosis)。EGFR-IN-196 可用于肺癌相关研究。

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EGFR-IN-196

EGFR-IN-196 Chemical Structure

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EGFR-IN-196 相关抗体

Top Publications Citing Use of Products

查看 EGFR 亚型特异性产品:

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EGFR/ErbB1/HER1 ErbB2/HER2 ErbB3/HER3 ErbB4/HER4

查看 PI3K 亚型特异性产品:

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PI3Kα PI3Kβ PI3Kγ PI3Kδ PI3KC2α PI3KC2β PI3KC2γ Vps34 PI3K PI3KC3 p120γ

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Akt Akt1 Akt2 Akt3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-196 is an EGFR inhibitor with an IC50 of 105.96 nM. EGFR-IN-196 inhibits EGFR enzymatic activity, reduces phosphorylated PI3K levels, and suppresses downstream EGFR-AKT signaling. EGFR-IN-196 increases intracellular ROS generation, induces mitochondrial depolarisation, and induces apoptosis in cancer cells. EGFR-IN-196 can be used for the research of lung cancer[1].

体外研究
(In Vitro)

EGFR-IN-196 (Compound 6E) 可抑制纯化的 EGFR 激酶，其 IC50 为 105.96 ± 0.45 nM[1]。
EGFR-IN-196 (1-25 μM; 24 h) 可抑制 A549 肺癌细胞增殖，其 IC50 为 4.355 ± 0.028 μM；且在 25 μM 作用 24 h 时对 HEK293 正常细胞无毒性[1]。
EGFR-IN-196 (5-30 min) 可时间依赖性地降低存活 A549 肺癌细胞中磷酸化 PI3K 的水平，从而抑制下游 EGFR 信号通路[1]。
EGFR-IN-196 (4.355 μM; 24 h) 可升高 A549 肺癌细胞内的 ROS 水平并破坏 A549 肺癌细胞的线粒体膜电位[1]。
EGFR-IN-196 (4.355 μM; 24 h) 可诱导 A549 肺癌细胞发生细胞凋亡，可观察到 19.6% 的早期凋亡细胞和 13.1% 的晚期凋亡细胞[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

EGFR-IN-196 相关抗体:

Apoptosis Analysis[1]

Cell Line: A549 lung cancer cells
Concentration: 4.355 μM
Incubation Time: 24 h
Result: Induced apoptotic cell death in A549 cells, with 19.6% early apoptotic cells and 13.1% late apoptotic cells detected by flow cytometry.
分子量

351.31

Formula

C18H11F2N5O
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

EGFR-IN-196 相关分类

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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.

Keywords:

EGFR-IN-196EGFRPI3KAktApoptosisReactive Oxygen Species (ROS)Mitochondrial MetabolismEpidermal growth factor receptorErbB-1HER1Phosphoinositide 3-kinasePKBProtein kinase BEGFR tyrosine kinase domainROSmitochondrial depolarisationHEK293lung cancerapoptoticA549AKTInhibitorinhibitorinhibit

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