DOTA-cTMTP1
DOTA-cTMTP1 is a cyclic tumor-homing peptide precursor molecule. DOTA-cTMTP1 selectively binds to XPNPEP2 on highly metastatic tumor cells, accumulates and retains in hepatocellular carcinoma tumors, and maintains a high tumor-to-liver contrast over time in small animal models. After radiolabeling with 68Ga, DOTA-cTMTP1 forms a PET probe for positron emission tomography (PET) imaging of hepatocellular carcinoma (HCC).
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- Formel: C55H92N20O21S2
- Molecular Weight:1433.57
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
Beschreibung
In Vitro
DOTA-cTMTP1 (20 μg; 10 min) exhibits > 99% radiolabeling efficiency when incubated with [68Ga]GaCl3 at 95 °C for 10 min, producing [68Ga]Ga-DOTA-cTMTP1 with a specific activity of 5.19 MBq/nmol[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
In Vivo
[68Ga]Ga-DOTA-cTMTP1 (i.v.; single dose) enables clear visualization of small HCC lesions in a transgenic mouse model, with increasing tumor-to-liver ratios over 120 min postinjection[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 (male, 5-6 weeks old, ~20 g)[1]
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Dosage:5.2 MBq
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Administration:i.v.; single dose
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Result:Reached tumor uptake of 1.3 %ID/g at 15 min, 1.09 %ID/g at 30 min, and 0.74 %ID/g at 150 min postinjection.
Showed tumor uptake of 0.98 %ID/g at 30 min with retention at later time points.
Achieved tumor-to-liver ratios of 2.65 at 30 min, 2.37 at 60 min, 2.14 at 120 min, and 2.69 at 150 min.
Reached tumor-to-muscle ratio of 11.17 at 150 min.
Reduced tumor uptake to 0.36 %ID/g at 30 min and 0.32 %ID/g at 60 min after coinjection of unlabeled TMTP1.
Decreased blood radioactivity from 1.11 %ID/g at 30 min to 0.48 %ID/g at 60 min, and then to 0.22 %ID/g at 120 min.
Chemical Information
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Molecular Weight 1433.57
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Formel C55H92N20O21S2
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Sequence
DOTA-Gly-Gly-Gly-Cys-Gly-Asn-Val-Val-Arg-Gln-Gly-Cys (Disulfide bridge: Cys1-Cys9)
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Sequence Shortening
DOTA-GGG-CGNVVRQGC (Disulfide bridge: Cys1-Cys9)
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Protokoll
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Liver Cancer Modeling
Liver cancer can be classified into primary liver cancer and secondary liver cancer. Secondary liver cancer is the metastatic liver cancer. Primary liver cancer includes hepatocellular carcinoma (HCC), intrahepatic cholangiocarcinoma (ICC) and fibrolamellar HCC, of which HCC is the most common form, accounting for approximately 90% of primary liver cancers[1]. HCC mouse models include chemical agent-induced models, transplanted tumor models, and genetic engineered models.
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Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
DOTA-cTMTP1 Related Classifications
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