2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK PI3K/Akt/mTOR
  3. EGFR Akt
  4. EGFR-IN-185

EGFR-IN-185 是一种 EGFR 抑制剂。EGFR-IN-185 对携带 EGFR 突变对非小细胞癌 (NSCLC) 细胞具有显著的抑制活性。EGFR-IN-185 可抑制克隆形成和迁移，诱导 G0/G1 期细胞阻滞，并促进细胞凋亡 (apoptosis)，这些作用均与 EGFR 和 AKT 磷酸化的抑制有关。EGFR-IN-185 可用于 NSCLC 研究。

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EGFR-IN-185

EGFR-IN-185 Chemical Structure

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EGFR-IN-185 相关抗体

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-185 is a EGFR inhibitor. EGFR-IN-185 exhibits potent activity against non-small cell lung cancer (NSCLC) cells harboring EGFR mutations. EGFR-IN-185 inhibits colony formation and migration, induces G0/G1 arrest, and promots apoptosis, which are associated with the suppression of EGFR and AKT phosphorylation. EGFR-IN-185 can be used for the research of  NSCLC[1].

体外研究
(In Vitro)

EGFR-IN-185 (compound 33) (48 小时) 对 NSCLC 细胞表现出抗增殖活性，IC50 分别为 3.1 (HCC827)、5.2 (H1975)、2.7 (H1975TM) 和 10.2 μM (A549)[1]。
EGFR-IN-185 (1-9 μM; 48 h) 以浓度依赖的方式将 H1975TM 细胞的细胞周期进程阻滞在 G0/G1 期[1]。
EGFR-IN-185 (0-10 μM；24 小时) 以浓度依赖对方式抑制 H1975TM 细胞的迁移[1]。
EGFR-IN-185 对 EGFRWT、EGFR19del、EGFRL858R/T790M 以及 EGFRL858R/T790M/C797S 均显示出可忽略不计的抑制活性，其 IC50 值分别为约 100、20、4 和 44 μM，这表明它并不作为变构 EGFR 酪氨酸激酶抑制剂起作用[1]。
EGFR-IN-185 (2-10 μM, 20 小时) 对 H1975TM 细胞表现出强烈的抗增殖效应，并能抑制 EGFR 信号通路，这一点通过 EGFR 和 AKT 磷酸化水平的降低得到证实[1]。
EGFR-IN-185 (0-9 μM, 10 天) 以浓度依赖的方式抑制了 H1975TM 细胞的集落形成[1]。
EGFR-IN-185 (2-8 μM, 32 小时) 通过浓度依赖性方式诱导细胞凋亡，从而抑制 H1975TM 细胞的生长[1]。

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

EGFR-IN-185 相关抗体:

Cell Cycle Analysis[1]

Cell Line: H1975™
Concentration: 1, 3, 6, and 9 μM
Incubation Time: 48 h
Result: Increased the percentage of H1975™ cells in the G0/G1 phase and decreased the S and G2/M phases. Increased the G0/G1 phase at 9 μM from 30.8% (control) to 59.7%, while it decreased S and G2/M phases from 50.3% and 18.9% to 31.1% and 9.3%, respectively.

Cell Migration Assay [1]

Cell Line: H1975™
Concentration: 0, 2, 4, 6, 10 μM
Incubation Time: 0, 12, and 24 h
Result: Inhibited H1975™ cell migration in a concentration-dependent manner. Exhibited only 12% and 22% wound closure at 10 μM after 12 and 24 h.

Western Blot Analysis[1]

Cell Line: H1975™
Concentration: 2, 6, and 10 μM
Incubation Time: 20 h
Result: Suppressed the phosphorylation of EGFR and its downstream proteins Akt in H1975™ cells in a concentration dependent manner. Significantly decreased the expression of p-EGFR by 59% and p-Akt by 57% at 10 μM. Did not target the downstream PI3Kα and AKT1 kinases of the EGFR pathway.

Cell Proliferation Assay[0]

Cell Line: H1975™
Concentration: 0, 1, 2, 4, 6, and 9 μM
Incubation Time: 10 days
Result: Inhibited colony formation of H1975™ cells in a concentration dependent manner. Exhibited a good inhibitory effect on the colony formation of H1975™ cells at concentrations above its IC₅₀ value (2.66 µM). Showed almost no colony formation at 9 μM.

Apoptosis Analysis[1]

Cell Line: H1975™
Concentration: 2, 6, and 8 μM
Incubation Time: 32
Result: Induced apoptosis in H1975™ cells in a concentration-dependent manner, increasing both early and late apoptotic populations. Increased the early and late apoptosis states at 8 μM from 1.11% and 2.51% (control) to 18.26% and 55.05%, respectively.
分子量

481.56

Formula

C30H28FN3O2
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-185 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-185EGFRAktEpidermal growth factor receptorErbB-1HER1PKBProtein kinase BH1975,NSCLC,EGFR-IN-185,EGFR,AKT,H1975?Inhibitorinhibitorinhibit

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