EGFR-IN-217
EGFR-IN-217 is an ATP-competitive EGFR kinase inhibitor, with an IC50 of 60.7 nM against EGFR. EGFR-IN-217 exhibits kinase inhibitory activity against PI3K-α and mTOR. EGFR-IN-217 upregulates pro-apoptotic factors including P53, Bax, PUMA, and caspase-7, -8 and -9, and downregulates the anti-apoptotic protein BCL-2, thereby inducing cell apoptosis and cycle arrest. EGFR-IN-217 shows tumor growth inhibitory effects in the solid Ehrlich ascites carcinoma xenograft mouse model. EGFR-IN-217 can be applied in the research of solid Ehrlich ascites carcinoma, hepatocellular carcinoma, and breast cancer.
For research use only. We do not sell to patients.
- Formula: C22H16BrNO3
- Molecular Weight:422.27
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
EGFR |
PI3Kα |
mTOR |
Caspase-7 |
Caspase-8 |
Caspase-9 |
Bax |
Bcl-2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
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| HepG2 | IC50 |
22.5 μM
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Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human hepatocellular carcinoma HepG2 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42594678 |
| MCF7 | IC50 |
12.0 μM
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Antiproliferative activity against human breast adenocarcinoma MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against human breast adenocarcinoma MCF-7 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42594678 |
| WI-38 | IC50 |
>100 μM
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Antiproliferative activity against normal human fetal lung fibroblast WI-38 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
Antiproliferative activity against normal human fetal lung fibroblast WI-38 cells assessed as reduction in cell viability incubated for 48 hrs by MTT assay.
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42594678 |
In Vitro
EGFR-IN-217 (0.001-100 μM) is a potent EGFR kinase inhibitor with an IC50 of 60.7 nM, and exhibits moderate secondary activity against PI3K-α and mTOR, the downstream effector molecules of the EGFR pathway[1].
EGFR-IN-217 (12 μM (IC50); 48 h) induces significant apoptotic cell death in MCF-7 breast adenocarcinoma cells and triggers cell cycle arrest at the G2/M phase[1].
EGFR-IN-217 (48 h) upregulates the pro-apoptotic genes P53, PUMA, BAX, caspase-7, caspase-8, and caspase-9, while downregulating the anti-apoptotic gene BCL-2, which confirms that it induces apoptosis via the intrinsic and extrinsic pathways in treated MCF-7 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MCF-7 and HepG2 cancer cell lines
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Concentration:6.25, 12.5, 25, 50, 100 μM
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Incubation Time:48 h
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Result:Exhibited potent antiproliferative activity against MCF-7 and HepG2 cancer cell lines, with high selectivity toward normal WI-38 cells, and showed an IC50 of 12.0 μM for MCF-7 cells and an IC50 of 22.5 μM for HepG2 cells.
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Cell Line:MCF-7 breast adenocarcinoma cells
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Concentration:12 μM
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Incubation Time:48 h
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Result:Induced apoptotic cell death.
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Cell Line:MCF-7 breast adenocarcinoma cells
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Concentration:12 μM
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Incubation Time:48 h
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Result:Triggered cell cycle arrest at the G2/M phase.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female immunocompetent BALB/c mice (6‑8 weeks old, 1 × 106 SEC solid Ehrlich carcinoma cells)[1]
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Dosage:6 mg/kg
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Administration:i.p.; 25 days
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Result:Suppressed tumor proliferation, improved hematological parameters and induced extensive tumor‑tissue necrosis (H&E staining).
- Annexin V plus membrane-impermeant dye apoptosis staining
- Patient-Derived Orthotopic Xenograft (PDOX)
- Liver Cancer Modeling
- Breast Cancer Modeling
- How to Choose the Right Model Animal
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Patient-Derived Xenograft (PDX)
- Apoptosis Solutions
- Splenic/Portal-Vein Liver Metastasis Xenograft
- Subcutaneous Cell-Line-Derived Xenograft
- Orthotopic Cell-Line Xenograft
- Intraperitoneal/Peritoneal Dissemination Xenograft
Chemical Information
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Molecular Weight 422.27
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Formula C22H16BrNO3
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SMILES
O=C1C=C(NC2=CC(Br)=CC=C2)OC(C1=C3)=CC=C3OCC4=CC=CC=C4
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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-217 Related Classifications
HY-189142 Related Classifications
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