2. JAK/STAT Signaling Protein Tyrosine Kinase/RTK Immunology/Inflammation
  3. EGFR PD-1/PD-L1
  4. 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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EP26 Chemical Structure

EP26 Chemical Structure

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EP26 Related Antibodies

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Description

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[1].

IC50 & Target[1]

EGFR

48.6 nM (IC50)

PD-L1

1.77 μM (IC50)

In Vitro

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.

EP26 Related Antibodies

Cell Proliferation Assay[1]

Cell Line: U87MG, U251, U87MG-vIII, GL261 cells
Concentration: 0-20 µM
Incubation Time: 72 h
Result: Showed antiproliferative activity with IC50s of 0.77, 1.02, 1.19, 0.28 µM for U87MG, U251, U87MG-vIII, GL261 cells, respectively.

Western Blot Analysis[1]

Cell Line: U87MG, U87vIII cells
Concentration: 0, 0.25, 1, 2 µM for U87MG cells, 0, 0.5, 1, 2, 4 µM
Incubation Time: 48 h
Result: Decreased the protein expression of p-EGFR in a dose-dependent manner.

Cell Cytotoxicity Assay[1]

Cell Line: U87MG cells
Concentration: 0.5, 1, 2 µM
Incubation Time: 48 h
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.
In Vivo

EP26 (50, 100 mg/kg; p.o.; once a day for 21 days) shows antitumor activity in mice[1]. Pharmacokinetic Parameters in Male SD rats[1].

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.

Animal Model: C57BL/6 mice (GL261 cells)[1]
Dosage: 50, 100 mg/kg
Administration: P.o.; once a day for 21 days
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.
Molecular Weight

737.26

Formula

C42H42ClFN4O5
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
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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EP26 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass   Concentration   Volume   Molecular Weight *
= × ×

The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • 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.

Keywords:

EP26EP 26EP-26EGFRPD-1/PD-L1Epidermal growth factor receptorErbB-1HER1PD-1/Programmed death-ligand 1orally activep-EGFRG0/G1 phaseU87MGU87vIII cellsglioblastomaanticancerInhibitorinhibitorinhibit

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