2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Epigenetics Stem Cell/Wnt Apoptosis Immunology/Inflammation NF-κB Metabolic Enzyme/Protease GPCR/G Protein Neuronal Signaling
  3. EGFR JAK Ferroptosis Apoptosis Reactive Oxygen Species (ROS) Cannabinoid Receptor Glutathione Peroxidase Caspase
  4. EGFR-IN-178

EGFR-IN-178 是一种口服有效的 EGFR 突变体抑制剂，对 EGFR 酶突变体具有高度选择性的抑制活性，包括Del19 (IC50 = 3.4 nM)、L858R/T790M (IC50 = 2.9 nM) 和 Del19/T790M (IC50 = 2.5 nM)。EGFR-IN-178 对 JAK2 (IC50 = 55.6 nM) 和JAK3 (IC50 = 46.1 nM) 激酶也具有良好的活性。EGFR-IN-178 能够增加细胞内脂质氧化物丙二醛 (MDA) 的含量，同时降低谷胱甘肽 (GSH) 的含量，最终导致癌细胞发生铁死亡 (ferroptosis)。EGFR-IN-178 通过增加裂解 caspase-3 的表达来促进细胞凋亡 (apoptosis)。EGFR-IN-178 能够抑制 EGFR 蛋白的磷酸化，降低 JAK2 的活性形式 p-JAK2，从而诱导细胞内活性氧 (ROS) 的增加。EGFR-IN-178 可用于非小细胞肺癌 (NSCLC) 的研究。

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EGFR-IN-178

EGFR-IN-178 Chemical Structure

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EGFR-IN-178 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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CB1 CB2

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GPX1 GPX4

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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-178 is an orally active EGFR mutant inhibitor, exhibits highly selective inhibitory activity against mutants of the EGFR enzyme, including Del19 (IC50 = 3.4 nM), L858R/T790 M (IC50 = 2.9 nM), and Del19/T790 M (IC50 = 2.5 nM). EGFR-IN-178 has good activity against JAK2 (IC50 = 55.6 nM) and JAK3 (IC50 = 46.1 nM) kinases. EGFR-IN-178 can increase cellular lipid oxide MDA, meanwhile decrease GSH content, causing ferroptosis in cancer cells. EGFR-IN-178 promotes apoptosis by increasing cleaved caspase-3 expression. EGFR-IN-178 can inhibit the phosphorylation of EGFR protein and decrease the active form p-JAK2 for JAK2, induce an increase in intracellular ROS. EGFR-IN-178 can be used for the study of non-small cell lung cancer (NSCLC)[1].

IC50 & Target

JAK2

55.6 nM (IC50)

JAK3

46.1 nM (IC50)

Caspase 3

 

体外研究
(In Vitro)

EGFR-IN-178 (1-100 nM，预处理 72 小时，随后培养 10-14 天) (Compound 14a) 对 H1975-EGFRL858R/T790M 细胞的 IC50 值为 18.5 nM，对 PC9-EGFRDel19 细胞的 IC50 值为 15.4 nM，在 5 nM 浓度下对 PC9-EGFRDel19 细胞显示出显著疗效，在约 10 nM 浓度下对 H1975-EGFRL858R/T790M 细胞显示出显著疗效，而即使在 100 nM 浓度下对 A549-EGFRWT 细胞也无抑制作用[1]。
EGFR-IN-178 (50-100 nM，24 小时) 可增强 H1975-EGFRL858R/T790M 细胞的绿色荧光，表明EGFR-IN-178 可导致细胞内活性氧 (ROS) 水平升高[1]。
EGFR-IN-178 (10-100 nM) 可抑制 H1975-EGFRL858R/T790M 细胞中 EGFR 的磷酸化，但不降低其总蛋白含量。该化合物通过显著降低浓度为 100 nM 时 p-JAK2 水平和浓度为 50 nM 时 p-STAT3 水平，同时抑制 JAK2-STAT3 信号通路，这与其对 JAK2-3 激酶活性的抑制作用一致[1]。
EGFR-IN-178 (5-100 nM，24 小时) 可诱导 H1975-EGFRL858R/T790M 细胞发生铁死亡，表现为脂质过氧化物 (MDA) 、铁离子 (Fe2+) 和氧化脂质水平升高，同时谷胱甘肽 (GSH) 和 GPX4 水平降低；此外，该化合物还通过增加裂解型 caspase-3 的表达促进细胞凋亡[1]。
EGFR-IN-178 (10-50 nM，12-24 小时) 能以浓度依赖的方式有效抑制 H1975-EGFRL858R/T790M 细胞的侵袭和迁移[1]。
EGFR-IN-178 对 HUVECs、HK-2、Hacat 以及小鼠来源的 C2C12 (肌肉组织) 和 NIH3T3 (胚胎成纤维细胞) 细胞均无明显毒性[1]。

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

EGFR-IN-178 相关抗体:

Cell Proliferation Assay[1]

Cell Line: A549 cells, PC9-EGFRDel19 cells, H1975-EGFRL858R/T790M
Concentration: 1 nM, 5 nM, 10 nM, 50 nM, 100 nM
Incubation Time: Pretreated for 72 hours, followed by culturing for 10–14 days
Result: Showed significant inhibition at 5 nM on PC9-EGFRDel19 cells, at approximately 10 nM on H1975-EGFRL858R/T790M cells, and no inhibition even at 100 nM on A549 cells.

Cell Invasion Assay[1]

Cell Line: H1975-EGFRL858R/T790M
Concentration: 10 nM, 50 nM
Incubation Time: 72 h
Result: Effectively inhibited the invasion of H1975-EGFRL858R/T790M cells.

Cell Migration Assay [1]

Cell Line: H1975-EGFRL858R/T790M
Concentration: 10 nM, 50 nM
Incubation Time: 12 h
Result: Effectively inhibited the migration of H1975-EGFRL858R/T790M cells.
体内研究
(In Vivo)

EGFR-IN-178 (10 mg/kg，口服，每日一次，持续 13 天) 在 H1975-EGFRL858R/T790M 荷瘤小鼠表现出强大的抗肿瘤活性，且无明显的体重减轻，精神状态、饮食或行为方面也无异常[1]。

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

Animal Model: Using a 1 mL sterile syringe, 0.2 mL of H1975-EGFRL858R/T790M cell suspension with a concentration of 5 × 10^7/mL was drawn and injected into the right armpit of each male nude mouse (4-week-old)[1].
Dosage: 10 mg/kg
Administration: P.o., once daily for 13 days
Result: Had a TGI of 90 % (tumor growth inhibition rate by weight).
No significant weight loss in the nude mice.
Mental state was normal, and no abnormalities in their eating and behavior.
分子量

463.54

Formula

C23H29N9O2
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-178 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-178EGFRJAKFerroptosisApoptosisReactive Oxygen Species (ROS)Cannabinoid ReceptorGlutathione PeroxidaseCaspaseEpidermal growth factor receptorErbB-1HER1Janus kinaseJak2-STAT-3 axisPyrazine derivativesInhibitorinhibitorinhibit

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