2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis Bcl-2 Family Caspase
  4. EGFR-IN-186

EGFR-IN-186 是一种强效的 EGFR 抑制剂，IC50 值为 0.065 µM。EGFR-IN-186 对 EGFRL858R (IC50 = 0.528 µM) 和 EGFRT790M (IC50 = 0.465 µM) 也具有抑制活性。EGFR-IN-186 通过增加 Bax 和 caspase-3 的水平并下调 Bcl-2 的表达水平来诱导细胞凋亡 (apoptosis)。EGFR-IN-186 可用于非小细胞肺癌 (NSCLC) 的研究。

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EGFR-IN-186

EGFR-IN-186 Chemical Structure

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EGFR-IN-186 相关抗体

Top Publications Citing Use of Products

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

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3 Bad

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Caspase 1 Caspase 2 Caspase 3 Caspase 4 Caspase 5 Caspase 6 Caspase 7 Caspase 8 Caspase 9 Caspase 10 Caspase 12 Caspase Caspase 11 Caspase-13

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-186 is a potent inhibitor of EGFR with an IC50 of 0.065 µM. EGFR-IN-186 also exhibits inhibitory activity against EGFRL858R (IC50 = 0.528 µM) and EGFRT790M (IC50 = 0.465 µM). EGFR-IN-186 induces apoptosis by increasing Bax and caspase-3 levels and down-regulating Bcl-2 expression level. EGFR-IN-186 can be used for the research of non-small cell lung cancer (NSCLC)[1].

IC50 & Target[1]

EGFR

0.065 μM (IC50)

EGFRL858R

0.528 μM (IC50)

EGFRT790M

0.465 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-186 (compound 6) (48 小时) 对 A549、NCI-H460 和 HOP-62 癌细胞系表现出强效的细胞毒性 (IC50 分别为 4.55、26.09 和 10.72 μM)，而对正常人肺成纤维细胞系 WI-38 的毒性则明显较低 (IC50 = 44.64 μM)[1]。
EGFR-IN-186 (48 小时) 对 A-549 细胞表现出增强的细胞毒性 (辐射后 IC50 = 2.38 μM)，表明其具有良好的放射增敏能力[1]。
EGFR-IN-186 (4.55 μM；48 小时) 通过增加 Bax 和 caspase-3 水平以及下调 A549 细胞中 Bcl-2 的表达水平来诱导细胞凋亡[1]。

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

EGFR-IN-186 相关抗体:

Apoptosis Analysis[1]

Cell Line: A-549
Concentration: 4.55 μM
Incubation Time: 48 h
Result: Caused a remarkable increase in early apoptosis from 0.79% (control) to 18.51%.
Showed an increase in the late cellular apoptosis from 0.18% (control) to 6.57%.
Induced early apoptosis in A-549 cells 1.65 folds better than Erlotinib (HY-50896).

ELISA Assay[1]

Cell Line: A-549
Concentration: 4.55 μM
Incubation Time: 48 h
Result: Increased the level of pro-apoptotic protein Bax expression compared to control.
Down-regulated the level of the expression of anti-apoptotic protein Bcl-2 compared to control.
Increased the Bax/BCl-2 ratio.
Led to activation of caspase-3 and increased its expression level when compared to untreated control cells.
分子量

472.52

Formula

C24H20N6O3S
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-186 相关分类

  • 摩尔计算器

  • 稀释计算器

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Help & FAQs
  • 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-186EGFRApoptosisBcl-2 FamilyCaspaseEpidermal growth factor receptorErbB-1HER1Lung cancerMolecular dockingInhibitorinhibitorinhibit

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