4-TCPA
4-TCPA is a potent VEGFR2 inhibitor. 4-TCPA induces apoptosis and cell cycle arrest, likely through inhibition of VEGFR2 and EGFR signaling with additional effects on the mTOR pathway. 4-TCPA can inhibit the vitality and proliferation of various cancer cell lines. 4-TCPA can be used for the study of cancers such as lung cancer, breast cancer and leukemia.
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- 分子式: C25H28ClN7O5
- 分子量:541.99
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
IC50 & Target
[1]|
VEGFR2 |
mTOR |
体外実験
4-TCPA (0-200 μM, 72 h) 4-TCPA exhibits inhibitory activity with IC50s of 35.70 μM for A549, 19.50 μM for MCF7, 5.95 μM for K562 and 135.2 μM for HFF2 cells[1].
4-TCPA (5.95-35.70 μM, 72 h) activates the mitochondrial pathway with varying sensitivity, causing apoptotic cell death in K562, MCF7 and A549 cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562, MCF7, A549 and HFF2 cells
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Concentration:5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200 μM
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Incubation Time:72 h
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Result:Demonstrated a dose- and time-dependent decrease in the viability and proliferation of cell lines.
Exhibited nearly twofold more activity in producing cytotoxic effects on the cancer cell line.
Was somewhat hazardous to the regular HFF2 cell line.
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Cell Line:K562, MCF7, A549 cells
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Concentration:5.95, 19.50, 35.70 μM
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Incubation Time:72 h
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Result:The early and late apoptosis in all cell lines increased significantly with time.
Observed more than 40% of the treated cells underwent apoptosis.
Increased the activity of caspase 3/7 in a time-dependent manner.
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Cell Line:K562, MCF7, A549 and HFF2 cells
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Concentration:5, 10, 15, 20, 30, 40, 50, 60, 70, 80, 90, 100, 150, 200 μM
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Incubation Time:72 h
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Result:Decreased the levels of EGFR, VEGFR2 and mTOR in A549.
Decreased the levels of EGFR, VEGFR2, mTOR, MAPK-1 and PIK3CA in MCF7.
Decreased the levels of EGFR, VEGFR2, mTOR, MAPK-1 and Akt in K562.
- Detection of Apoptosis
- TUNEL staining for apoptotic DNA fragmentation
- Flow cytometric DNA-content cell-cycle staining
- Annexin V plus membrane-impermeant dye apoptosis staining
- BrdU Incorporation Assay
- Apoptosis Solutions
- Protocol for Cell Cycle
- Breast Cancer Modeling
- Cell Viability Determination by MTT Colorimetric Assay
化学情報
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分子量 541.99
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分子式 C25H28ClN7O5
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SMILES
O=C(NC1=CC=C(Cl)C=C1)CN2N=NC(CNC3=C4C=C(OCCOC)C(OCCOC)=CC4=NC=N3)=C2
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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)