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.
- Formula: C40H56ClNO6
- Molecular Weight:682.33
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Biological Activity
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EGFR 5.19 μM (IC50) |
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.
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Cell Line:HCT-116 cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:48 h
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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.
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Cell Line:HCT-116 cells
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Concentration:2.5, 5 and 10 μM
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Incubation Time:24 and 48 h
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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.
| Species | Dose | Route | Tmax | Cmax | T1/2 | AUC0-t |
|---|---|---|---|---|---|---|
| Rat[1] | 20 mg/kg | i.p. | 6.0 h | 19.89 ng/mL | 1.89 h | 164.11 ng·h/mL |
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.
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Animal Model:CT-26 tumor mice models[1]
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Dosage:5 and 10 mg/kg
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Administration:Intraperitoneally injection
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Result:Significantly reduced tumor weight.
Had no effect on body weight.
Showed a significantly reduced proportion of proliferative marker Ki-67.
Chemical Information
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Molecular Weight 682.33
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Formula C40H56ClNO6
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
EGFR-IN-169 Related Classifications
HY-175531 Related Classifications
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