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.
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- 分子式: C22H16BrNO3
- 分子量:422.27
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
製品説明
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 |
体外実験
EGFR-IN-217 (compound 4v) (6.25-100 μM; 48 h) exhibits potent antiproliferative activity against MCF-7 and HepG2 cancer cell lines, with high selectivity toward normal WI-38 cells, and shows an IC50 of 12.0 μM for MCF-7 cells and an IC50 of 22.5 μM for HepG2 cells[1].
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.
体内実験
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).
化学情報
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分子量 422.27
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分子式 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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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
EGFR-IN-217 関連分類
HY-189142 関連分類
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