NOTA-PTP
NOTA-PTP is an aggregation agent and imaging agent targeting Plectin-1. NOTA-PTP achieves targeted accumulation in Plectin-1-expressing cells and tumors. NOTA-PTP accumulates in a time-dependent manner in pancreatic ductal adenocarcinoma cells. NOTA-PTP serves as a precursor for the synthesis of [68Ga]Ga-NOTA-PTP, a Plectin-1-targeted positron emission tomography radiotracer for pancreatic ductal adenocarcinoma imaging. NOTA-PTP can be used in studies related to pancreatic ductal adenocarcinoma.
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- Fòrmula: C50H89N13O14
- Peso molecular:1096.32
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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
NOTA-PTP (0-200 μg/mL; 24 h) shows no significant cytotoxicity in CFPAC-1, KPC, and MIN-6 cell lines at concentrations up to 200 μg/mL after 24 h of incubation[1].
NOTA-PTP (10-12-10-5 M; 60 min) inhibits the binding of [68Ga]Ga-NOTA-PTP to plectin-1 with an IC50 of 12.8 nM in CFPAC-1 cells and 15.3 nM in KPC cells[1].
Unlabeled NOTA-PTP (1000-fold molar excess; 10-120 min) specifically inhibits the uptake of [68Ga]Ga-NOTA-PTP in plectin-1-expressing CFPAC-1 and KPC cells, and produces a smaller inhibition in low-plectin-1 MIN-6 cells, confirming target-specific binding[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
[68Ga]Ga-NOTA-PTP (7.4-9.6 MBq, 0.925-1.11 MBq; i.v.) accumulates in plectin-1-expressing KPC pancreatic cancer xenografts with peak uptake of 2.69 %ID/g at 0.5 h postinjection, and achieves favorable tumor-to-background ratios by 1.5 h postinjection[1].
[68Ga]Ga-NOTA-PTP (7.4-9.6 MBq, 0.925-1.11 MBq; i.v.) exhibits minimal accumulation in plectin-1-low-expressing MIN-6 pancreatic cancer xenografts, with peak uptake of 0.69 %ID/g at 0.5 h postinjection[1].
[68Ga]Ga-NOTA-PTP (7.4-9.6 MBq; i.v.) enables clear visualization of orthotopic pancreatic tumors and peritoneal metastases in KPC mice at 45 min postinjection, with superior diagnostic contrast compared to 2-[18F]FDG[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:BALB/c nude (female, 18−20 g, subcutaneous xenograft via inoculation of 5 × 10^6 CFPAC-1 cells)[1]
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Dosage:7.4−9.6 MBq (imaging); 0.46 μmol (unlabeled NOTA-PTP for blocking studies)
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Administration:i.v.
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Result:Visualized tumors distinctly as early as 0.5 h postinjection, with tumor uptake measured at 1.65 %ID/g, which decreased to 0.86 %ID/g at 90 min.
Significantly reduced tumor uptake to 0.35 %ID/g at 1 h postinjection when excess unlabeled NOTA-PTP was coadministered.
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Animal Model:C57BL/6 (18−20 g, subcutaneous xenograft via inoculation of 2.5 × 10^6 KPC cells)[1]
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Dosage:7.4−9.6 MBq (imaging); 0.925−1.11 MBq (biodistribution studies)
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Administration:i.v.
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Result:Showed significant tracer accumulation in tumors, with uptake of 1.75 %ID/g at 30 min postinjection via PET imaging.
Measured tumor uptake of 2.69 %ID/g at 0.5 h, 1.53 %ID/g at 1 h, and 0.91 %ID/g at 1.5 h via biodistribution analysis.
Achieved tumor-to-normal organ ratios at 1.5 h: tumor/muscle 4.38, tumor/liver 1.30, tumor/kidney 0.18, tumor/heart 2.66, and tumor/blood 3.32.
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Animal Model:BALB/c nude (female, 18−20 g, subcutaneous xenograft via inoculation of 5 × 10^6 MIN-6 cells)[1]
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Dosage:7.4−9.6 MBq (imaging); 0.925−1.11 MBq (biodistribution studies)
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Administration:i.v.
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Result:Showed minimal tracer accumulation in tumors, with uptake of 0.44 %ID/g at 30 min postinjection via PET imaging.
Measured tumor uptake of 0.69 %ID/g at 0.5 h, 0.37 %ID/g at 1 h, and 0.32 %ID/g at 1.5 h via biodistribution analysis.
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Animal Model:C57BL/6 (18−20 g, orthotopic and peritoneal metastasis model via injection of 1 × 10^8 KPC cells/mL into pancreatic parenchyma)[1]
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Dosage:7.4−9.6 MBq
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Administration:i.v.
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Result:Clearly visualized both orthotopic pancreatic tumors and small peritoneal metastases with high tumor-to-background contrast via PET imaging at 45 min postinjection.
Chemical Information
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Peso molecular 1096.32
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Fòrmula C50H89N13O14
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Sequence
Lys-Thr-Leu-Leu-Pro-Thr-Pro-{EDA}-{NOTA}
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Sequence Shortening
KTLLPTP-{EDA}-{NOTA}
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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)
NOTA-PTP Related Classifications
HY-P11849 Related Classifications
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