PJ27
PJ27 is a dual PD-1/PD-L1/JAK1 inhibitor, with an IC50 of 414 nM against PD-1/PD-L1, an IC50 of 786 nM against JAK1, a Ka of 294 nM for human PD-1/PD-L1, and a Ka of 473 nM for murine PD-1/PD-L1. PJ27 promotes the infiltration of CD3+CD8+ and CD3+CD4+ cells into the tumor microenvironment and exerts a significant immune activation effect. PJ27 inhibits tumor growth in a dose-dependent manner in the LLC lung cancer mouse model. PJ27 is applicable to relevant research on lung cancer.
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- Fòrmula: C38H40N8O2
- Peso molecular:640.78
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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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Chemical Information
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Actividad biológica
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JAK3 786 nM (IC50) |
PJ27 (0.125-2 μM; 48 h) enhances Jurkat T cell-mediated killing of PD-L1-expressing A549 cells, with significant A549 viability reduction at 2 μM in co-culture[1].
PJ27 binds to human and murine PD-L1 with comparable affinity, with Kd values of 294 nM and 473 nM respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A549, Jurkat T cells
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Concentration:0, 0.125, 0.25, 0.5, 1, 2 μM
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Incubation Time:48 h
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Result:Showed almost no inhibitory activity against A549 or Jurkat T cells cultured alone.
Significantly decreased A549 cell viability at 2 μM in co-culture model.
Enhanced Jurkat T cell-mediated killing of A549 cells in co-culture model.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (male, 5 to 6 weeks old, subcutaneous inoculation of 1 × 106 LLC cells)[1]
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Dosage:25 mg/kg; 50 mg/kg
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Administration:i.p.; daily; 11 days
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Result:Achieved a tumor growth inhibition rate (TGI) of 21% and reduced phosphorylated STAT3 (p-STAT3) levels in tumor tissues compared to control at 25 mg/kg.
Achieved a TGI of 56%, reduced p-STAT3 and PD-L1 levels in tumor tissues, increased the percentage of CD3+CD8+ cytotoxic T cells in tumor tissues to 38.8% (vs.
16.3% in control), and increased the percentage of CD3+CD4+ helper T cells in tumor tissues to 50.5% (vs.
28.9% in control) at 50 mg/kg.
Showed no significant body weight loss or organ toxicity in either dose group.
Chemical Information
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Peso molecular 640.78
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Fòrmula C38H40N8O2
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SMILES
CC1=C(C2=NC(OC)=C(CNC3CCN(C(CCCN4C=C(C5=NC=NC6=C5C=CN6)C=N4)=O)CC3)C=C2)C=CC=C1C7=CC=CC=C7
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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)
PJ27 Related Classifications
HY-181663 Related Classifications
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