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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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CyGbPF

CyGbPF Chemical Structure

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Description

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[1].

In Vitro

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.

In Vivo

CyGbPF (10 μM/kg; intravenous injection; single administration) generates localized, activation-dependent NIRF signals in breast cancer mice, which correlate with the level of immune activation; non-invasive tracking of graded immune activation is achievable via tumor NIRF imaging and optical urine analysis[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Balb/c (tumor-bearing, implanted with 4T1 breast cancer cells, pretreated with immunotherapeutic agents for immunoactivation)[1]
Dosage: 10 μM/kg
Administration: i.v.; single dose
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.
Molecular Weight

3367.84

Formula

C163H273IN8O56

SMILES

CC[C@@H]([C@@H](C(N[C@H](C([C@H](CC1=CC=CC=C1)N[C@H](C(NC2=CC=C(C=C2)COC3=CC(OC4=C5/C=C/C(C(C)(C6=CC=CC=C67)C)=[N+]7CCCCN8C=C(COCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOC)N=N8)=C(C=C4CCC5)C=C3)=O)CC(OC(C)(C)C)=O)=O)CCC(OC(C)(C)C)=O)=O)NC(C)=O)C.[I-]

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Please store the product under the recommended conditions in the Certificate of Analysis.

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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.

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CyGbPF
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