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AGI-43192 Sale

目录号 : GC64635

AGI-43192 是一种有效的蛋氨酸腺苷转移酶 2A (MAT2A) 抑制剂。AGI-43192 是一种有效但有限的脑渗透化合物。AGI-43192 具有探索 SAM 调节在中枢神经系统 (CNS) 中的作用和癌症疾病研究的潜力。

AGI-43192 Chemical Structure

Cas No.:2377491-54-6

规格 价格 库存 购买数量
5 mg
¥3,150.00
现货
10 mg
¥5,040.00
现货
25 mg
¥10,170.00
现货

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Sample solution is provided at 25 µL, 10mM.

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产品描述

AGI-43192 is a potent inhibitor of methionine adenosyltransferase 2A (MAT2A). AGI-43192 is a potent, but limited brain-penetrant compound. AGI-43192 has the potential for exploring the effects of SAM modulation in the central nervous system (CNS) and research of cancer disease[1].

[1]. Li M, et al. Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads. J Med Chem. 2022;65(6):4600-4615.

Chemical Properties

Cas No. 2377491-54-6 SDF Download SDF
分子式 C23H16ClF3N6O 分子量 484.86
溶解度 DMSO : 83.33 mg/mL (171.86 mM; ultrasonic and warming and heat to 60°C) 储存条件 Store at -20°C
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.0625 mL 10.3123 mL 20.6245 mL
5 mM 0.4125 mL 2.0625 mL 4.1249 mL
10 mM 0.2062 mL 1.0312 mL 2.0625 mL
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Research Update

Leveraging Structure-Based Drug Design to Identify Next-Generation MAT2A Inhibitors, Including Brain-Penetrant and Peripherally Efficacious Leads

J Med Chem 2022 Mar 24;65(6):4600-4615.PMID:35293760DOI:10.1021/acs.jmedchem.1c01595

Inhibition of the S-adenosyl methionine (SAM)-producing metabolic enzyme, methionine adenosyltransferase 2A (MAT2A), has received significant interest in the field of medicinal chemistry due to its implication as a synthetic lethal target in cancers with the deletion of the methylthioadenosine phosphorylase (MTAP) gene. Here, we report the identification of novel MAT2A inhibitors with distinct in vivo properties that may enhance their utility in treating patients. Following a high-throughput screening, we successfully applied the structure-based design lessons from our first-in-class MAT2A inhibitor, AG-270, to rapidly redesign and optimize our initial hit into two new lead compounds: a brain-penetrant compound, AGI-41998, and a potent, but limited brain-penetrant compound, AGI-43192. We hope that the identification and first disclosure of brain-penetrant MAT2A inhibitors will create new opportunities to explore the potential therapeutic effects of SAM modulation in the central nervous system (CNS).