|AGI-24512|CsnPharm

CAS No.: 2201066-53-5

AGI-24512 Catalog No. CSN22342

AGI-24512 is a methionine adenosyltransferase 2A (MATA2 ) inhibitors useful for treatment of cancer. AGI-24512 blocks growth of MTAP-deleted cancer cells in vitro.

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400-920-2911

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技术信息

生物活性

描述MAT2A (Methionine Adenosyltransferase 2A) catalyzes the production of S-adenosyl methionine (AdoMet; SAM) from methionine and ATP. AdoMet is the propylamino donor in polyamine biosynthesis and the principal methyl donor for DNA methylation and is involved in gene transcription and cellular proliferation. In hepatocellular carcinoma (HCC), up-regulation of MAT2A was reported to occur, resulting in lower AdoMet contents, which may provide a growth advantage to hepatoma cells. According to a report, MAT2A inhibition may be a potential therapy in MTAP (Methylthioadenosine Phosphorylase) deleted cancers. MTAP is another important gene in metabolism^[1]. AGI-24512 is a MATA2 inhibitor, inhibiting MAT2A activity to a content of approximately 100% at the concentration of 1 μM. In HCT116 cells, AGI-24512 inhibited the production of S-adenosyl methionine, with the IC50 of 103 nM. In MTAP deleted background, AGI-24512 dose dependently suppressed the level of SDMA, with the IC50 of 95.2 nM, suggesting that MAT2A inhibition impacts PRMT5 activity in this setting{{Targeting MAT2A in MTAP-deleted Cancers|http://investor.agios.com/static-files/6f86f736-a23c-4c9c-b455-81c1ac1128f9}}.
作用机制AGI-24512 is a MATA2 inhibitor. According to cocrystal study of the enzyme and the inhibitor, AGI-24512 binds in allosteric site and impacts conformation of the active site gate loop{{Targeting MAT2A in MTAP-deleted Cancers|http://investor.agios.com/static-files/6f86f736-a23c-4c9c-b455-81c1ac1128f9}}.
参考文献

[1] Marjon K, Cameron MJ, Quang P, Clasquin MF, Mandley E, Kunii K, McVay M, Choe S, Kernytsky A, Gross S, Konteatis Z, Murtie J, Blake ML, Travins J, Dorsch M, Biller SA, Marks KM. MTAP Deletions in Cancer Create Vulnerability to Targeting of the MAT2A/PRMT5/RIOK1 Axis. Cell Rep. 2016 Apr 19;15(3):574-587.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.4970 mL
- 12.4852 mL
- 24.9705 mL
- 5 mM
- 0.4994 mL
- 2.4970 mL
- 4.9941 mL
- 10 mM
- 0.2497 mL
- 1.2485 mL
- 2.4970 mL

技术信息

CAS号	2201066-53-5	储存条件	粉末液体 -20°C:3-6 月 -80°C:12月
分子式	C24H24N4O2	运输	蓝冰
分子量	400.47	别名

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