2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR kinase inhibitor 1

EGFR kinase inhibitor 1 是一种有效的 EGFR 抑制剂，对 WT, l885R/T790M, L858R/T790M/C797S 的 IC50 分别为 37、1.7、>300 nM。EGFR kinase inhibitor 1 诱导细胞凋亡 (apoptosis) 和细胞周期停滞在 G0/G1 期。EGFR kinase inhibitor 1 抑制细胞转移。EGFR kinase inhibitor 1 具有抗增殖和抗肿瘤活性。

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EGFR kinase inhibitor 1 Chemical Structure

EGFR kinase inhibitor 1 Chemical Structure

CAS No. : 2413958-04-8

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EGFR kinase inhibitor 1 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

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR kinase inhibitor 1 is a potent EGFR inhibitor with IC50s of 37, 1.7, >300 nM for WT, l885R/T790M, L858R/T790M/C797S, respectively. EGFR kinase inhibitor 1 induces apoptosis and cell cycle arrest at G0/G1-phase. EGFR kinase inhibitor 1 inhibits the cell motility. EGFR kinase inhibitor 1 shows antiproliferative and anti-tumor activity[1].

IC50 & Target[1]

EGFR (WT)

37 nM (IC50)

EGFRL858R/T790M

1.7 nM (IC50)

EGFRL858R/T790M/C797S

>300 nM (IC50)

体外研究
(In Vitro)

EGFR kinase inhibitor 1 (compound 17i) (72 h) shows antiproliferative activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively[1].
EGFR kinase inhibitor 1 (0.05, 0.5, 5 µM; 48 h) induces apoptosis in a dose-dependent manner[1].
EGFR kinase inhibitor 1 (4, 20, 100 nM; 48 h) induces cell cycle arrest at G0/G1-phase[1].
EGFR kinase inhibitor 1 (0.5 μM; 0, 24, 48 h) inhibits the motility of the H1975 cells[1].

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

EGFR kinase inhibitor 1 相关抗体:

Cell Cytotoxicity Assay[1]

Cell Line: A549, H1975 cells
Concentration:
Incubation Time: 72 h
Result: Showed antiproliferation activity with IC50s of 4.17, 0.052 µM for A549, H1975 cells, respectively.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 0.05, 0.5, 5 µM
Incubation Time: 48 h
Result: Induced apoptosis in a dose-dependent manner.

Apoptosis Analysis[1]

Cell Line: H1975 cells
Concentration: 4, 20, 100 nM
Incubation Time: 48 h
Result: Induced cell cycle arrest at G0/G1-phase with the percentage of G0/G1-phase cells increased from 42.93% to 60.52% at 4 nM, 70.39% at 20 nM and 80.03% at 100 nM.
分子量

521.61

Formula

C30H31N7O2
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

EGFR kinase inhibitor 1 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 kinase inhibitor 12413958-04-8EGFR kinase inhibitor1EGFR kinase inhibitor-1EGFRApoptosisEpidermal growth factor receptorErbB-1HER1antiproliferativeanti-tumorapoptosisG0/G1-phaseH1975 cellscell motilityInhibitorinhibitorinhibit

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