CyGbPF
CyGbPF is a granzyme B-specific near-infrared fluorescent probe. CyGbPF can be cleaved by granzyme B to remove the peptide cage group, restoring near-infrared fluorescence. CyGbPF passively accumulates in mouse tumors, and its activated fluorescence correlates with granzyme B expression, CD8+ cytotoxic T lymphocyte populations, and CD4+ helper T lymphocyte populations in tumor tissues. CyGbPF is efficiently cleared by the kidneys, enabling the assessment of immune activation via optical urine analysis. CyGbPF allows real-time non-invasive evaluation of cancer immunotherapeutic efficacy in living animals. CyGbPF can be used in research on cancers such as breast cancer. Excitation wavelength/emission wavelength: approximately 658 nm/approximately 717 nm.
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- 분자량:2000 (Average)
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
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Biological Activity
CyGbPF (2-250 μM; 5-90 min) is specifically cleaved by mouse granzyme B in cell-free assays, exhibiting a 24-fold near-infrared fluorescence enhancement[1].
CyGbPF (5 μM; 0.5-2.0 h; 1.60-200 μg/mL) is rapidly activated by endogenous granzyme B in CD8+ T cells, with a time-dependent fluorescence enhancement amplitude approximately 35-fold higher than that in 4T1 cells and approximately 15-fold higher than that in RAW264.7 cells; moreover, it exhibits only extremely low cytotoxicity at concentrations up to 200 μg/mL across all three cell lines[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Balb/c (tumor-bearing, implanted with 4T1 breast cancer cells, pretreated with immunotherapeutic agents for immunoactivation)[1]
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Dosage:10 μM/kg
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Administration:i.v.; single dose
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Result:Reached maximum tumor NIRF signal intensity at 6 hours post-injection.
Showed tumor NIRF signals 1.47-fold (NLG919-pretreated), 1.54-fold (R848-pretreated), 2.23-fold (BMS-1-pretreated), 2.79-fold (pexidartinib-pretreated), and 2.85-fold (BEC-pretreated) higher than control mice at 6 hours post-injection.
Accumulated 14% of injected dose in tumors with negligible accumulation in other organs.
Correlated strongly with tumor tissue levels of granzyme B, CD8+ T cells, and CD4+ T cells, which were elevated in immunotherapy-treated mice relative to controls.
Chemical Information
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분자량 2000 (Average)
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SMILES
CC(N[C@@H]([C@H](CC)C)C(N[C@H](C(N[C@H](C(N[C@H](C(NC1=CC=C(C=C1)COC2=CC(OC3=C4/C=C/C(C(C)(C5=CC=CC=C56)C)=[N+]6CCCCN7C=C(COCCOC)N=N7)=C(C=C3CCC4)C=C2)=O)CC(O)=O)=O)CC8=CC=CC=C8)=O)CCC(O)=O)=O)=O.[I-].[n]
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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