ES3-JFTN
ES3-JFTN is an EGFR inhibitor. ES3-JFTN inhibits the TGF-β1/SMAD2 signaling pathway and downregulates FOXP3. Upon binding to EGFR, ES3-JFTN exhibits environment-sensitive turn-on fluorescence, enabling tumor-selective imaging, and mainly localizes to mitochondria in cells. ES3-JFTN inhibits tumor growth in a syngeneic mouse model of colon cancer. ES3-JFTN can be used for research on colon cancer.
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- Fòrmula: C31H33ClFN9O5
- Peso molecular:666.10
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
FOXP3 |
TGF-β1/SMAD2 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| MCF7 | IC50 |
70.11 μM
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Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human MCF-7 cells assessed as viability reduction incubated 72 hrs by MTT assay.
|
5432962 |
| MDA-MB-231 | IC50 |
3.98 μM
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Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human MDA-MB-231 cells assessed as viability reduction incubated 72 hrs by MTT assay.
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5432962 |
| HT-29 | IC50 |
13.42 μM
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Antiproliferative activity against human HT-29 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human HT-29 cells assessed as viability reduction incubated 72 hrs by MTT assay.
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5432962 |
| HCT-116 | IC50 |
1.93 μM
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Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human HCT-116 cells assessed as viability reduction incubated 72 hrs by MTT assay.
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5432962 |
| CT26 | IC50 |
1.37 μM
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Antiproliferative activity against CT-26 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against CT-26 cells assessed as viability reduction incubated 72 hrs by MTT assay.
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5432962 |
| HepG2 | IC50 |
1.97 μM
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Antiproliferative activity against human HepG-2 cells assessed as viability reduction incubated 72 hrs by MTT assay.
Antiproliferative activity against human HepG-2 cells assessed as viability reduction incubated 72 hrs by MTT assay.
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5432962 |
In Vitro
ES3-JFTN (2.5-20 μM) fluorescence tracks EGFR expression, showing higher signal in EGFR-high MDA-MB-231 and HCT-116 cells than in EGFR-low MCF-7 and HT-29 cells[1].
ES3-JFTN localizes predominantly to mitochondria and co-localizes with EGFR in HCT-116 and HT-29 cells[1].
ES3-JFTN (5-20 μM; 24 h) inhibits EGFR phosphorylation and suppresses the TGF-β1/SMAD2 pathway in HCT-116 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT-116 cells
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Concentration:5, 15, 20 μM
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Incubation Time:24 h
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Result:Significantly inhibited EGFR phosphorylation and TGF-β1 activation.
Reduced expression of TGF-β1, p-SMAD2, and SMAD2 was observed.
Densitometric analysis confirmed these inhibitory effects.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c (male, 5-7 weeks, 25-30 g)[1]
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Dosage:5 mg/kg
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Administration:i.p.; every 48 h; four total administrations
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Result:Exhibited a tumor growth inhibition rate of 77.69% in the CT-26 model.
By the end of the experiment, the average tumor volume was approximately 200 mm3.
In tumor tissues, the lowest proportion of TI-Tregs and the highest proportion of CD8+ T cells were observed compared to the gefitinib and PBS groups; in contrast, the proportion of peripheral Tregs (P-Tregs) in peripheral blood and spleens remained unchanged.
TGF-β1/SMAD2 signaling was suppressed in tumor tissues, with reduced expression of TGF-β1, p-SMAD2, and SMAD2.
No significant changes in body weight or major organs were observed.
Chemical Information
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Peso molecular 666.10
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Fòrmula C31H33ClFN9O5
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SMILES
FC(C=C1)=C(Cl)C=C1NC2=NC=NC3=CC(OC)=C(OCCCN4CCN(CCCNC5=CC=C([N+]([O-])=O)C6=NON=C56)CC4)C=C32
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
ES3-JFTN Related Classifications
HY-189846 Related Classifications
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