EGFR-IN-214
EGFR-IN-214 is an orally active EGFR inhibitor with an EC50 of 3.353 μM. EGFR-IN-214 blocks the downstream PI3K/Akt signaling pathway, induces intracellular ROS accumulation and Caspase-dependent apoptosis. EGFR-IN-214 exhibits antiproliferative activity in cancer cells and inhibits tumor growth in xenograft models. EGFR-IN-214 can be used in studies related to hepatocellular carcinoma.
For research use only. We do not sell to patients.
- CAS No.: 3077316-17-4
- Formula: C39H37F3N2O11
- Molecular Weight:766.71
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
EGFR-IN-214 (0.5-4 μM; 72 h) potently inhibits the viability of HepG2 (IC50 = 2.20 μM) and Huh7 (IC50 = 1.16 μM) human hepatocellular carcinoma cells in vitro[1].
EGFR-IN-214 (0.05-0.4 μM; continuous incubation for colony formation) potently suppresses the colony-forming ability of HepG2 and Huh7 human hepatocellular carcinoma cells in a concentration-dependent manner[1].
EGFR-IN-214 (0.5-4 μM; 72 h) induces caspase-dependent mitochondrial apoptosis in HepG2 and Huh7 human hepatocellular carcinoma cells in vitro in a concentration-dependent manner[1].
EGFR-IN-214 (0.5-4 μM; 72 h) disrupts mitochondrial redox homeostasis by inducing robust concentration-dependent accumulation of intracellular ROS and mitochondrial superoxide in HepG2 and Huh7 human hepatocellular carcinoma cells[1].
EGFR-IN-214 (0.5-4 μM; 72 h) suppresses the EGFR/PI3K/Akt signaling pathway in HepG2 and Huh7 human hepatocellular carcinoma cells by reducing EGFR phosphorylation and total EGFR levels, leading to downstream inhibition of PI3K and AKT phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HepG2 and Huh7 cells
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Concentration:0.5, 1 and 2 μM (Huh7 cells); 1, 2 and 4 μM (HepG2 cells)
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Incubation Time:72 h
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Result:Induced caspase-dependent mitochondrial apoptosis.
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Cell Line:HepG2 and Huh7 cells
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Concentration:0.5, 1 and 2 μM (Huh7 cells); 1, 2 and 4 μM (HepG2 cells)
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Incubation Time:72 h
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Result:Increased Bax, Cleaved Caspase-3.
Reduced Bcl-2, p-EGFR/Total EGFR, p-PI3K/p-Akt and p-ERK.
| Species | Dose | Route | T1/2 | Vss | CL | AUC |
|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 13.46 h | 167.36 L/kg | 0.15 L/min/kg | 69.5 mg/min/L |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (male, 5 weeks old, subcutaneously inoculated with 5×106 Huh7 cells)[1]
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Dosage:15 mg/kg; 30 mg/kg
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Administration:i.g.; every other day; 14 days
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Result:Showed potent, dose-dependent tumor growth suppression compared to vehicle control.
Demonstrated improved antitumor efficacy relative to positive control Icaritin at 30 mg/kg.
Significantly reduced EGFR-positive area and Ki67-positive area in tumor tissues.
Maintained stable body weight throughout the study.
Caused no obvious histopathological abnormalities in major organs (heart, liver, spleen, lung, kidney) and organ indices comparable to control.
Chemical Information
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CAS No. 3077316-17-4
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Molecular Weight 766.71
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Formula C39H37F3N2O11
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SMILES
O=C1C(O[C@H]2[C@H](O)[C@H](O)[C@@H](O)[C@H](C)O2)=C(C3=CC=C(OC)C=C3)OC4=C1C(O)=CC(OCC5=NN=C(/C=C/C6=CC=C(C(F)(F)F)C=C6)O5)=C4C/C=C(C)\C
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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-214 Related Classifications
HY-184311 Related Classifications
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