MAT2A ligand 1
MAT2A ligand 1 is a MAT2A ligand inhibitor (IC50=29.5 nM) and PET tracer that crosses the blood-brain barrier. MAT2A ligand 1 enables non-invasive imaging of MAT2A-expressing tumors, with rapid tumor uptake equilibrium, a high tumor-to-muscle ratio, and specific tumor-binding properties. MAT2A ligand 1 is applicable to research related to non-small cell lung cancer, hepatocellular carcinoma, colorectal cancer, gastric cancer, glioblastoma, pancreatic adenocarcinoma, urothelial carcinoma, breast cancer, and prostate cancer.
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- Formule: C18H18ClFN4O2
- Masse moléculaire:376.81
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
[18F]MAT2A ligand 1 ([18F]1d) (1 μCi/mL; 5-120 min) is specifically taken up by H1975 cells via binding to MAT2A, with an internalization rate of 46%, and shows a relatively fast efflux rate (the efflux rate reaches 70% at 120 min)[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:Multiple solid tumors model in BALB/c nude (female, 6-8 weeks old, 12-16 g, subcutaneous xenograft of A549/PC-3/22RV1/MCF-7/MDA-MB-231/DU145 cells)[1]
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Dosage:3.7-7.4 MBq/100 μL
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Administration:Intravenous tail injection;22Rv1, A549, DU145, MCF-7, MDA-MB-231, and PC-3 subcutaneous tumor at 1 h and 2 h post-treatment; measured at 60 and 120 min
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Result:Achieved tumor uptake values of 4.06 ± 0.37 %ID/g (22RV1), 3.86 ± 0.42 %ID/g (A549), 4.11 ± 0.36 %ID/g (DU145), 4.56 ± 0.29 %ID/g (MCF-7), 3.16 ± 0.45 %ID/g (MDA-MB-231), and 4.1 ± 0.11 %ID/g (PC-3) at 1 hour post-injection.
Showed generally comparable tumor-to-muscle ratios across all six models, with only MDA-MB-231 having slightly lower tumor uptake.
Showed no positive correlation between tumor uptake and MAT2A expression levels across the models.
Chemical Information
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Masse moléculaire 376.81
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Formule C18H18ClFN4O2
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SMILES
O=C1N(C2=C(C(N(C)CCOCCF)=N1)C=CC(Cl)=C2)C3=CC=NC=C3
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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