AGW-11
AGW-11 is a potent dual inhibitor of EGFR (IC50 = 556 nM) and VEGFR2 (IC50 = 289.7 nM). AGW-11 induces apoptosis and suppresses phosphorylation of EGFR, VEGFR2, and ERK1/2 in HUVECs. AGW-11 effectively inhibits cancer cell growth, reduces HUVEC proliferation, tube formation, and invasion, thereby blocking angiogenesis. AGW-11 significantly suppresses tumor growth and decreases lung metastasis in a 4T1 xenograft mouse model. AGW-11 can be used for the study of breast cancer.
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- Formule: C31H36N2O6
- Masse moléculaire:532.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
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VEGFR2 289.7 nM (IC50) |
EGFR 556 nM (IC50) |
AGW-11 (0.5-30 μM, 48 h) exhibits potent antiproliferative activity against MDA-MB-231, 4T1, A2780, and HCT-116 cancer cells, with IC50 values of 1.26 μM, 2.85 μM, 0.75 μM, and 1.58 μM, respectively[1].
AGW-11 (0.5-2 μM, 24 h) significantly inhibits the phosphorylation of EGFR and ERK1/2 in MDA-MB-231 cells in a concentration-dependent manner[1].
AGW-11 (2 μM, 24 h) potently inhibits colony formation and induces apoptosis in 4T1 breast cancer cells[1].
AGW-11 (1-4 μM, 6-24 h) potently suppresses tube formation of HUVECs and exerts concentration-dependent inhibitory activity on HUVEC invasion[1].
AGW-11 (1-4 μM, 24 h) effectively reduces the phosphorylation of VEGFR2 and ERK1/2 in n HUVECs in a concentration-dependent manner[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:MDA-MB-231 cells
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Concentration:0.5, 1. 2 μM
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Incubation Time:24 h
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Result:Inhibited the phosphorylation of EGFR and ERK1/2 in MDA-MB-231 cells in a concentration-dependent manner.
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Cell Line:4T1 breast cancer cells
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Concentration:2 μM
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Incubation Time:24 h
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Result:Induced apoptosis in 4T1 breast cancer cells.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:4T1 mouse breast cancer cells (1×106 cells per mouse) were subcutaneously inoculated into the dorsal region of 4-6-week-old female BALB/c mice (18-20 g body weight)[1]
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Dosage:1 mg/kg and 5 mg/kg
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Administration:i.p., once every 2 days, 20 days
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Result:Achieved tumor volume reduction rates of 34.5% and 32.4% at doses of 1 mg/kg and 5 mg/kg.
Showed no significant changes in body weight.
Reduced the Ki67 expression and reduced the CD31 and VEGF expressions.
Decreased the phosphorylation of VEGFR2 and its downstream molecule ERK1/2.
Increased the level of cleaved caspase 3.
Reduced the number of metastatic lung nodules.
Enhanced tumor necrosis and inhibited abnormal transformation of liver and lung tissues.
Chemical Information
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Masse moléculaire 532.63
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Formule C31H36N2O6
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SMILES
CC(OC[C@]([C@]1([H])[C@@]([C@H](C/C=C2C(OC[C@@H]/2OC3=C4N=CC=CC4=CC=C3)=O)C(CC1)=C)(C)CC5)(C)NC5=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
AGW-11 Related Classifications
HY-175820 Related Classifications
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