EP26
EP26 is a potent and orally active EGFR and PD-L1 inhibitor with IC50 values of 48.6 nM, 1.77 µM, respectively. EP26 decreased the protein expression of p-EGFR. EP26 induces cell cycle arrest at G0/G1 phase. EP26 has the potential for the research of glioblastoma.
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- Fòrmula: C42H42ClFN4O5
- Peso molecular:737.26
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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EGFR 48.6 nM (IC50) |
PD-L1 1.77 μM (IC50) |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| U-251 | IC50 |
1.02 μM
Compound: EP26
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Antiproliferative activity against human U-251 cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human U-251 cells incubated for 72 hrs by MTT assay
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[PMID: 38739112] |
| U-87MG ATCC | IC50 |
0.77 μM
Compound: EP26
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Antiproliferative activity against human U-87 MG cells incubated for 72 hrs by MTT assay
Antiproliferative activity against human U-87 MG cells incubated for 72 hrs by MTT assay
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[PMID: 38739112] |
EP26 (0-4 µM; 48 h) decreases the protein expression of p-EGFR in a dose-dependent manner[1].
EP26 (0.5, 1, 2µM; 48 h) induces cell cycle arrest at G0/G1 phase[1].
EP26 binds binds to human PD-L1 and murine PD-L1 in a dose-dependent manner with KDs of 0.58, 0.52 µM, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:U87MG, U251, U87MG-vIII, GL261 cells
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Concentration:0-20 µM
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Incubation Time:72 h
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Result:Showed antiproliferative activity with IC50s of 0.77, 1.02, 1.19, 0.28 µM for U87MG, U251, U87MG-vIII, GL261 cells, respectively.
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Cell Line:U87MG, U87vIII cells
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Concentration:0, 0.25, 1, 2 µM for U87MG cells, 0, 0.5, 1, 2, 4 µM
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Incubation Time:48 h
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Result:Decreased the protein expression of p-EGFR in a dose-dependent manner.
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Cell Line:U87MG cells
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Concentration:0.5, 1, 2 µM
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Incubation Time:48 h
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Result:Induced cell cycle arrest at G0/G1 phase with the percentage of U87MG cells in G0/G1 phase increased from 60.51 to 63.57, 69.48, and 73.98%, respectively.
| PK parameters | i.v. administration (4 mg/kg, n = 5) | p.o. administration (20 mg/kg, n = 5) |
| AUC(0-t) (µg/L*h) | 2832.5 ± 954.8 | 3145.7 ± 778.7 |
| AUC(0-∞) (µg/L*h) | 2906.6 ± 1061.8 | 3238.3 ± 752.2 |
| MRT(0-t) (h) | 12.7 ± 0.8 | 17.5 ± 1.6 |
| MRT(0-∞) (h) | 2906.6 ± 1061.8 | 3238.3 ± 752.2 |
| t1/2 (h) | 6.8 ± 3.7 | 13.0 ± 5.3 |
| Tmax (h) | 0.04 ± 0.02 | 3.6 ± 0.9 |
| Vz (L/kg) | 13.7 ± 4.4 | 123.5 ± 64.6 |
| CL (L/h/kg) | 1.5 ± 0.6 | 6.4 ± 1.3 |
| Cmax (µg/L) | 325.6 ± 166.8 | 255.3 ± 123.0 |
| F(%) | - | 22.2 |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice (GL261 cells)[1]
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Dosage:50, 100 mg/kg
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Administration:P.o.; once a day for 21 days
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Result:Decreased the tumor weight and tumor volume by 92.0 and 89.7% at 100 mg/kg, significantly inhibited glioblastoma tumor growth with tumor growth inhibitions (TGIs) of 61.4%, 89.4% at 50, 100 mg/kg, respectively.
Chemical Information
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Peso molecular 737.26
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Fòrmula C42H42ClFN4O5
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SMILES
COC1=CC(OCC2=C(C)C(C3=CC=CC=C3)=CC=C2)=CC(OC)=C1CNCCCCOC4=C(OC)C=C(N=CN=C5NC6=CC=CC(Cl)=C6F)C5=C4
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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)
EP26 Related Classifications
HY-159101 Related Classifications
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