1. Epigenetics Metabolic Enzyme/Protease
  2. Methionine Adenosyltransferase (MAT)
  3. MAT2A ligand 1

MAT2A ligand 1 是一种 MAT2A 配体抑制剂 (IC50=29.5 nM) 与 PET 示踪剂,可透过血脑屏障。MAT2A ligand 1 可用于对表达 MAT2A 的肿瘤进行无创成像,具有快速的肿瘤摄取平衡、较高的肿瘤-肌肉比值、特异性肿瘤结合特性。MAT2A ligand 1 可用于非小细胞肺癌、肝细胞癌、结直肠癌、胃癌、胶质母细胞瘤、胰腺腺癌、尿路上皮癌、乳腺癌、前列腺癌的相关研究。

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MAT2A ligand 1

MAT2A ligand 1 Chemical Structure

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

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[1].

体外研究
(In Vitro)

[18F]MAT2A ligand 1 ([18F]1d) (1 μCi/mL; 5-120 min) 可通过与 MAT2A 结合被 H1975 细胞特异性摄取,其内化率为 46%,且外排速度相对较快 (120 min 时外排率达 70%)[1]

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

体内研究
(In Vivo)

[18F]MAT2A ligand 1 ([18F]1d) (3.7-7.4 MBq/100 μL; 尾静脉注射) 在多种表达 MAT2A 的实体瘤异种移植模型中实现了稳定的肿瘤摄取,尽管摄取水平与 MAT2A 表达无直接相关性,但仍验证了其在 MAT2A 靶向 PET 成像中的广泛适用性[1]

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

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]
Dosage: 3.7-7.4 MBq/100 μL
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
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.\n
Showed generally comparable tumor-to-muscle ratios across all six models, with only MDA-MB-231 having slightly lower tumor uptake.\n
Showed no positive correlation between tumor uptake and MAT2A expression levels across the models.
分子量

376.81

Formula

C18H18ClFN4O2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

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

纯度 & 产品资料
参考文献
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  • 稀释计算器

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  • 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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MAT2A ligand 1
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HY-181285
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