2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR-IN-165

EGFR-IN-165 是一种强效的 EGFR 抑制剂。EGFR-IN-165 对激酶 EGFRL858R/T790M 和 EGFRWT 的 IC50 值分别为 17.18 和 64.74 nM，对 NCI-H1975 细胞和 A431 细胞的 IC50 值分别为 2.17 和 6.2 μM。EGFR-IN-165 显著抑制细胞迁移，诱导细胞停滞于 G1 期，引起细胞凋亡 (apoptosis)。EGFR-IN-165 可用于研究诸如非小细胞肺癌、结直肠癌以及头颈部鳞状细胞癌等癌症。

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EGFR-IN-165

EGFR-IN-165 Chemical Structure

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EGFR-IN-165 相关抗体

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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-165 is a potent EGFR inhibitor. EGFR-IN-165 demonstrates superior potency with IC50s of 17.18 and 64.74 nM against EGFRL858R/T790M and EGFRWT; 2.17 and 6.2 μM against NCI-H1975 cells and A431 cells. EGFR-IN-165 significantly inhibits the migration and induces G1 phase cell cycle arrest and cell apoptosis. EGFR-IN-165 can be used for the study of cancers such as non-small cell lung cancer, colorectal cancer, and head and neck squamous cell carcinoma[1].

体外研究
(In Vitro)

EGFR-IN-165 (Compound 4b) (0-5 μM, 48 h) 以浓度依赖的方式有效抑制 A431 和 NCI-H1975 细胞中的 EGFR 磷酸化[1]。
EGFR-IN-165 (1.25-10 μM, 24 h) 在浓度为 10 μM 时有效抑制 A431 细胞的迁移[1]。
EGFR-IN-165 (2.5-20 μM, 48 h) 在浓度为 20 μM 时，在 NCI-H1975 细胞中达到 12.91% 的凋亡率[1]。
EGFR-IN-165 (2.5-20 μM, 24-48 h) 使 NCI-H1975 细胞在 G1 期发生细胞周期停滞[1]。
EGFR-IN-165 在人体血浆中具有极高的稳定性，半衰期为 38.5 h，在肝微粒体中的清除率极低，其内在清除率为 24.3 mL/min/kg[1]。

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

EGFR-IN-165 相关抗体:

Western Blot Analysis[1]

Cell Line: A431 and NCI-H1975 cells
Concentration: 0, 1.25, 2.5, 5 μM
Incubation Time: 48 h
Result: Demonstrated significant and concentration-dependent inhibition of EGFR phosphorylation in A431 cells.
Exhibited effective and concentration-dependent inhibition of EGFR phosphorylation.

Cell Migration Assay [1]

Cell Line: A431 cells
Concentration: 1.25, 2.5, 5 and 10 μM
Incubation Time: 24 h
Result: Effectively inhibited the migration at a concentration of 10 μM.

Apoptosis Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 48 h
Result: Reached 12.91% apoptosis rate in NCI-H1975 cells at a concentration of 20 μM.

Cell Cycle Analysis[1]

Cell Line: NCI-H1975 cells
Concentration: 2.5, 5, 10 and 20 μM
Incubation Time: 24-48 h
Result: The proportion of the G1 phase increased to 73.09 %, while the S phase decreased to 17.29 % and the G2 phase to 9.48 %.
分子量

483.48

Formula

C26H21N5O5
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-165 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-165EGFRApoptosisEpidermal growth factor receptorErbB-1HER11,3,4-oxadiazoleCancerActivity evaluationA431 cellsNCI-H1975 cellsInhibitorinhibitorinhibit

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