PD-1/PD-L1-IN-69
PD-1/PD-L1-IN-69 is an orally active PD-L1 dimerization inducer and FAK phosphorylation inhibitor (IC50 = 18.7 nM for human PD-1/PD-L1 interaction). PD-1/PD-L1-IN-69 blocks the PD-1/PD-L1 interaction by stabilizing dimerization within the PD-L1 dimerization pocket, and inhibits VEGF-A-induced FAK phosphorylation and angiogenesis, thereby enhancing immune-mediated tumor cell death. PD-1/PD-L1-IN-69 can be used for research on colon adenocarcinoma.
For research use only. We do not sell to patients.
- Formula: C26H24INO3
- Molecular Weight:525.38
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All VEGFR Isoforms
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Biological Activity
Description
IC50 & Target
[1]|
PD-1/PD-L1 18.7 nM (IC50) |
In Vitro
PD-1/PD-L1-IN-69 (3-6 μM; 24 h) inhibits VEGF-A-induced HUVEC migration[1].
PD‑1/PD‑L1‑IN‑69 (6 μM; 24 h) produces anti‑angiogenic and anti‑migratory effects in HUVECs associated with reduced FAK phosphorylation[1].
PD-1/PD-L1-IN-69 (6 μM; 24 h) decreases total FAK expression in VEGF-A-stimulated HUVEC cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HCT116 and MC38 cells
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Concentration:0.625, 1.25, 2.5, 5, 10 μM
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Incubation Time:48 h
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Result:Showed minimal cytotoxicity against HCT116 monocultures at 10 μM with 93% viability.
Induced superior tumor cell death in the coculture system with 70% viability.
Demonstrated dose-dependent cytotoxicity against MC38 cells with 86% and 72% viability at 2.5 and 5 μM respectively.
Enhanced MC38 cell death by 20% in coculture versus monoculture at 5 μM.
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Cell Line:HUVECs
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Concentration:6 μM
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Incubation Time:24 h (treatment); 6 h (incubation on Matrigel)
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Result:Markedly suppressed VEGF-A-induced tube formation.
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Cell Line:HUVECs
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Concentration:3, 6 μM
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Incubation Time:24 h
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Result:Significantly attenuated VEGF-A-induced migration at 6 μM.
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Cell Line:HUVECs
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Concentration:6 μM
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Incubation Time:24 h
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Result:Notably reduced phosphorylation of FAK without affecting total FAK levels.
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Cell Line:HUVEC cells
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Concentration:6 μM
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Incubation Time:24 h
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Result:Reduced total FAK expression in VEGF-A-stimulated HUVEC cells.
Parmacokinetics
In Vivo
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 (male, 6−8 weeks old, 18−22 g)[1]
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Dosage:30; 60 mg/kg
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Administration:i.g.; daily; 14 days
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Result:Sustained intragastric administration of QA9 was well tolerated, with no significant alterations in body weight or observable adverse effects.
QA9 exhibited pronounced dose-dependent antitumor activity.
At the higher dose (60 mg/kg), QA9 administration resulted in substantial reductions in tumor volume (75%) and tumor weight (79%), demonstrating superior efficacy compared to NP19 (65 and 70%, respectively) at an equivalent dosage.
The lower dose (30 mg/kg) also elicited significant antitumor effects, with reductions of 57% in tumor volume and 66% in tumor weight relative to vehicle-treated controls.
Histopathological assessment via H&E staining revealed intact cellular architecture and absence of necrosis across multiple organ systems in both treatment groups.
Flow cytometric analysis of tumor-infiltrating lymphocytes showed that QA9 treatment elevated activated helper T cells (CD3+ CD4+: 2.5%) and cytotoxic T cells (CD3+ CD8+: 7.8%) compared to the vehicle control (1.2 and 3.5%, respectively).
- Kinase activity and phosphorylation assays
- Western Blot
- Human pluripotent stem cell endothelial-cell differentiation
- Vascular/Branching Fractal Analysis
- Cell Cytotoxicity Assay
- Mammalian live/dead viability and cytotoxicity staining
- Endothelial Tube Formation Assay
- Apoptosis Solutions
- Protocol for Kinase activity and phosphorylation assays
- Endothelial Cell Migration/Angiogenic Sprouting Assay
Chemical Information
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Molecular Weight 525.38
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Formula C26H24INO3
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SMILES
CC1=C(C2=CC3=C(C=[N+](CCO)C=C3)C=C2)C=CC=C1C4=CC5=C(C=C4)OCCO5.[I-]
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Keywords
- PD-1/PD-L1-IN-69
- PD-1/PD-L1
- FAK
- VEGFR
- VEGF-A-induced FAK phosphorylation
- endothelial cell migration
- HUVECs
- tumor-infiltrating T-cell activation
- PD-1/PD-L1 protein-protein interaction
- angiogenesis
- colon adenocarcinoma
- FAK phosphorylation inhibitor
- PD-L1 dimerization inducer
- endothelial tube formation
- Inhibitor
- inhibitor
- inhibit