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

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.

For research use only. We do not sell to patients.

EGFR-IN-169

EGFR-IN-169 Chemical Structure

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EGFR-IN-169 Related Antibodies

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Description

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)

In Vitro

EGFR-IN-169 (Compound 4e) shows IC50 values of 4.46 μM for HCT-116, 6.89 μM for CT-26, 9.03 μM for HT-29, 16.01 μM for SW620 and 18.98 μM for Caco-2 cells[1].
EGFR-IN-169 (5-10 μM, 48 h) inhibits the clonal formation in HCT-116 and CT-26 cell lines[1].
EGFR-IN-169 (2.5-10 μM, 48 h) induces significant G0/G1 phase arrest in HCT-116 cells[1].
EGFR-IN-169 (2.5-10 μM, 24-48 h) induces apoptosis in HCT-116 cells[1].
EGFR-IN-169 (2.5-10 μM, 12 h) induces mitochondrial damage and ROS accumulation in HCT-116 cells[1].
EGFR-IN-169 (5 μM, 48 h) inhibits migration and invasion in HCT-116 cells[1].
EGFR-IN-169 (2.5-10 μM) inhibits the activation of RalA protein in a dose-dependent manner in HCT-116 cells[1].

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

EGFR-IN-169 Related Antibodies

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.
In Vivo

EGFR-IN-169 (Compound 4e) (100 mg/kg, daily dor 7-14 days) shows a good safety profile in mice[1].
EGFR-IN-169 (5-10 mg/kg, i.p., a single dose) inhibits tumor growth in CT-26 tumor mice models[1].

MedChemExpress (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.
Molecular Weight

682.33

Formula

C40H56ClNO6
SMILES

O=C(C1=C(N2CC(O[C@@H]3C(C)(C)C(CC[C@]4(C)C5CC(O)C6[C@@]4(C)CCC6[C@@]7(C)CCCC(C)(C)O7)[C@]5(C)CC3)=O)C(Cl)=CC=C1)C2=O
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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EGFR-IN-169 Related Classifications

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Help & FAQs
  • 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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