2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis PI3K/Akt/mTOR Stem Cell/Wnt MAPK/ERK Pathway
  3. EGFR Apoptosis Akt ERK
  4. EGFR-IN-120

EGFR-IN-120 (Compound 11eg) 是一种口服有效的 EGFR 抑制剂。EGFR-IN-120 抑制 EGFRL858R/T790M/C797S 突变体的 IC50 值为 0.053 μM，对 EGFRWT 的作用相对较弱 (IC50: 1.05 μM)。EGFR-IN-120 抑制 EGFR 和主要下游效应物 (STAT3、AKT 和 Erk) 的磷酸化。EGFR-IN-120 在 EGFR 突变细胞中诱导细胞周期停滞和细胞凋亡 (Apoptosis)。 EGFR-IN-120 抑制含有 EGFRL858R/T790M/C797S 突变体的 NSCLC 细胞的增殖，IC50 为 0.052 μM。

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EGFR-IN-120 Chemical Structure

EGFR-IN-120 Chemical Structure

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EGFR-IN-120 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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Akt Akt1 Akt2 Akt3

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ERK ERK1 ERK2 ERK5 ERK8

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-120 (Compound 11eg) is an orally active EGFR inhibitor. EGFR-IN-120 inhibits EGFRL858R/T790M/C797S with an IC50 value of 0.053 μM, and has a relatively weak effect on EGFRWT (IC50: 1.05 μM). EGFR-IN-120 inhibits the phosphorylation of EGFR and main downstream effectors (STAT3, AKT, and Erk). EGFR-IN-120 induces cell cycle arrest and cell apoptosis in EGFR mutant cells. EGFR-IN-120 inhibits the proliferation of the NSCLC cells harboring EGFRL858R/T790M/C797S with an IC50 of 0.052 μM[1].

IC50 & Target[1]

EGFRL858R/T790M/C797S

0.053 μM (IC50)

分子量

570.66

Formula

C31H35FN8O2
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-120 相关分类

  • 摩尔计算器

  • 稀释计算器

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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-120EGFRApoptosisAktERKEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BExtracellular signal regulated kinasesEGFR mutantNSCLCInhibitorinhibitorinhibit

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