2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis
  3. EGFR Apoptosis
  4. EGFR-IN-172

EGFR-IN-172 是一种 EGFR 抑制剂。EGFR-IN-172 能有效抑制携带 L858R、T790M 和 C797S 药物耐药突变的非小细胞肺癌 (NSCLC) 细胞的增殖。EGFR-IN-172 可抑制 EGFR 的磷酸化，诱导细胞周期停滞和细胞凋亡 (apoptosis)。EGFR-IN-172 可用于 NSCLC 的研究。

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EGFR-IN-172

EGFR-IN-172 Chemical Structure

CAS No. : 878416-74-1

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EGFR-IN-172 相关抗体

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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-IN-172 is a EGFR inhibitor. EGFR-IN-172 effectively inhibits the proliferation of non-small cell lung cancer (NSCLC) cells carrying the L858R, T790M and C797S drug-resistant mutations. EGFR-IN-172 inhibits EGFR phosphorylation, induces cell cycle arrest and apoptosis. EGFR-IN-172 can be used for the study of NSCLC[1].

体外研究
(In Vitro)

EGFR-IN-172 (Compound 2b) 对 A549 细胞 (EGFRWT) (IC50 = 5.31 μM)、PC-9 细胞 (EGFRT790M) (IC50 = 0.55 μM)、H1975 细胞 (EGFRL858R/T790M) (IC50 = 0.40 μM) 和 Ba/F3-EGFRL858R/T790M/C797S 细胞 (IC50 = 2.36 μM) 表现出较高的抗增殖活性[1]。
EGFR-IN-172 (0.1-10 μM) 可抑制EGFR (pEGFR) 在 H1975 和 Ba/F3 三重突变细胞中以浓度依赖性方式发挥作用[1]。
EGFR-IN-172 (0.25-1 μM, 48 h) 将 H1975 细胞阻滞于 G0/G1 期，但对 Ba/F3 三重突变细胞的细胞周期没有显著影响[1]。
EGFR-IN-172 (0.25-1 μM, 48 h) 以浓度依赖性方式诱导 H1975 和 Ba/F3 三重突变细胞凋亡[1]。

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

EGFR-IN-172 相关抗体:

Cell Cycle Analysis[1]

Cell Line: ​H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 48 h
Result: Arrested H1975 cells in the G0/G1 phase of the cell cycle.
Did not affect Ba/F3-EGFRL858R/T790M/C797S cells.

Apoptosis Analysis[1]

Cell Line: ​H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 48 h
Result: Effectively induced apoptosis in two EGFR mutant lung cancer cells.

Western Blot Analysis[1]

Cell Line: ​H1975 and Ba/F3-EGFRL858R/T790M/C797S cells
Concentration: 0.25, 0.5 and 1 μM
Incubation Time: 48 h
Result: Inhibited the phosphorylation of EGFR in a concentration-dependent manner in both cell lines.
分子量

359.40

Formula

C22H18FN3O
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-IN-172 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-172878416-74-1EGFRApoptosisEpidermal growth factor receptorErbB-1HER1C797S mutationL858R/T790M mutationNSCLCInhibitorinhibitorinhibit

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