1. Protein Tyrosine Kinase/RTK Stem Cell/Wnt MAPK/ERK Pathway Apoptosis JAK/STAT Signaling
  2. VEGFR ERK Apoptosis EGFR
  3. 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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AGW-11

AGW-11 Chemical Structure

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Description

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[1].

IC50 & Target[1]

VEGFR2

289.7 nM (IC50)

EGFR

556 nM (IC50)

In Vitro

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.

Western Blot Analysis[1]

Cell Line: MDA-MB-231 cells
Concentration: 0.5, 1. 2 μM
Incubation Time: 24 h
Result: Inhibited the phosphorylation of EGFR and ERK1/2 in MDA-MB-231 cells in a concentration-dependent manner.

Apoptosis Analysis[1]

Cell Line: 4T1 breast cancer cells
Concentration: 2 μM
Incubation Time: 24 h
Result: Induced apoptosis in 4T1 breast cancer cells.
In Vivo

AGW-11 (1-5 mg/kg, i.p., once every 2 days, 20 days) exhibits significant anti-tumor activity in BALB/c mice bearing 4T1 breast tumor xenografts[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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]
Dosage: 1 mg/kg and 5 mg/kg
Administration: i.p., once every 2 days, 20 days
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.
Molecular Weight

532.63

Formula

C31H36N2O6

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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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AGW-11
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HY-175820
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