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.
For research use only. We do not sell to patients.
- Formula: C18H18ClFN4O2
- Molecular Weight:376.81
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Protocols
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
In Vitro
[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. Further protocols information, click here.
In Vivo
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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Molecular Weight 376.81
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Formula 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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Cell Cytotoxicity Assay
Cytotoxicity assays are usually based on the assessment of cell membrane damage, which can also be indirectly detected by measuring cell viability. Detection methods include MTT assay, CKK-8 assay, LDH assay and ATP assay, etc.
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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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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MAT2A ligand 1 Related Classifications
HY-181285 Related Classifications
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