2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Apoptosis NF-κB Metabolic Enzyme/Protease Immunology/Inflammation Cell Cycle/DNA Damage
  3. EGFR Apoptosis Reactive Oxygen Species (ROS) CDK Bcl-2 Family
  4. EGFR-IN-169

EGFR-IN-169 是一种源自人参二醇的表皮生长因子 (EGFR) 抑制剂，其 IC50 值为 5.19 μM。EGFR-IN-169 通过抑制 EGFR 介导的 RalA/EMT 通路，来干扰结直肠癌细胞的迁移和生长。EGFR-IN-169 对 HCT-116 细胞的 IC50 值为 4.46 μM，选择指数 (SI) 为 16.92。EGFR-IN-169 会抑制 CDKs 活性，诱导 G0/G1 期细胞周期停滞，并抑制细胞迁移和侵袭。EGFR-IN-169 能降低线粒体膜电位，诱导细胞凋亡 (apoptosis) 和活性氧 (ROS) 的产生。EGFR-IN-169 可用于癌症研究，例如结直肠癌。

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EGFR-IN-169

EGFR-IN-169 Chemical Structure

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EGFR-IN-169 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

查看 CDK 亚型特异性产品:

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CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK8 CDK9 CDK11 CDK12 CDK13 CDK14 CDK16 CDK19 CDC CLK Pho85 CDK10 CDK15 CDK17 CDK18 CDK20 PITSLRE

查看 Bcl-2 Family 亚型特异性产品:

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Bcl-2 Bcl-xL Bcl-W Mcl-1 Bfl-1 Bcl-B Bax Bak Bim BNIP3

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

EGFR-IN-169 is an epidermal growth factor (EGFR) (IC50 = 5.19 μM) inhibitor form panaxadiol. EGFR-IN-169 interferes with the migration and growth of colorectal cancer cells by inhibiting EGFR-mediated RalA/EMT pathway. EGFR-IN-169 shows an IC50 value of 4.46 μM and SI of 16.92 for HCT-116 cells. EGFR-IN-169 inhibits CDKs activity, induces G0/G1 cycle arrest and inhibits migration and invasion. EGFR-IN-169 reduces mitochondrial membrane potential and induces apoptosis and ROS production. EGFR-IN-169 can be used for the research of cancer, such as colorectal cancer[1].

IC50 & Target

EGFR

5.19 μM (IC50)

体外研究
(In Vitro)

EGFR-IN-169 (Compound 4e) 对 HCT-116 细胞的 IC50 值为 4.46 μM，对 CT-26 细胞为 6.89 μM，对 HT-29 细胞为 9.03 μM，对 SW620 细胞为 16.01 μM，对 Caco-2 细胞为 18.98 μM[1]。
EGFR-IN-169 (5-10 μM, 48 h) 可抑制 HCT-116 和 CT-26 细胞系的集落形成[1]。
EGFR-IN-169 (2.5-10 μM, 48 h) 可诱导 HCT-116 细胞显著发生 G0/G1 期阻滞[1]。
EGFR-IN-169 (2.5-10 μM, 24-48 h) 可诱导 HCT-116 细胞凋亡[1]。
EGFR-IN-169 (2.5-10 μM, 12 h) 可诱导 HCT-116 细胞发生线粒体损伤和活性氧 (ROS) 积累[1]。
EGFR-IN-169 (5 μM, 48 h) 可抑制 HCT-116 细胞的迁移和侵袭[1]。
EGFR-IN-169 (2.5-10 μM) 可在 HCT-116 细胞中以剂量依赖的方式抑制 RalA 蛋白的激活[1]。

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

EGFR-IN-169 相关抗体:

Cell Cycle Analysis[1]

Cell Line: HCT-116 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 48 h
Result: Induced significant G0/G1 phase arrest.
Decreased cells in the S phase and G2/M phase.
Downregulated the expression of CDK2, CDK4, CDK6, and Cyclin D1.

Apoptosis Analysis[1]

Cell Line: HCT-116 cells
Concentration: 2.5, 5 and 10 μM
Incubation Time: 24 and 48 h
Result: Enhanced membrane permeability and promoted a time-dependent shift from early to late apoptosis.
Reduced Bcl-2 levels and increased Bax levels.
Increased γ-H2AX expression.
体内研究
(In Vivo)

EGFR-IN-169 (Compound 4e) (100 mg/kg，每日一次，持续 7-14 天) 在小鼠中显示出良好的安全性[1]。
EGFR-IN-169 (5-10 mg/kg，腹腔注射) 在 CT-26 肿瘤小鼠模型中可抑制肿瘤生长[1]。

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

Animal Model: CT-26 tumor mice models[1]
Dosage: 5 and 10 mg/kg
Administration: Intraperitoneally injection
Result: Significantly reduced tumor weight.
Had no effect on body weight.
Showed a significantly reduced proportion of proliferative marker Ki-67.
分子量

682.33

Formula

C40H56ClNO6
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-169 相关分类

  • 摩尔计算器

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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-169EGFRApoptosisReactive Oxygen Species (ROS)CDKBcl-2 FamilyEpidermal growth factor receptorErbB-1HER1Cyclin dependent kinasePanaxadiolHCT-116RalA/EMTROSColorectal cancerInhibitorinhibitorinhibit

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