AGI-24512
目录号: PL07101 纯度: ≥99%
CAS No. :2201066-53-5
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中文名称
AGI-24512
英文名称
AGI-24512
英文别名
BCP29872;AGI 24512; AGI24512;6-(4-hydroxyphenyl)-5-methyl-2-phenyl-3-(piperidin-1-yl)pyrazolo[1,5-a]pyrimidin-7(4H)-one;6-(4-Hydroxyphenyl)-5-methyl-2-phenyl-3-piperidin-1-yl-1H-pyrazolo[1,5-a]pyrimidin-7-one;AGI-24512
Cas No.
2201066-53-5
分子式
C24H24N4O2
分子量
400.47
包装储存
Powder -20°C 3 years;In solvent -80°C 6 months
产品详情
AGI-24512 是一种蛋氨酸腺苷转移酶 2α (MAT2A) 抑制剂,IC50 为 8 nM。AGI-24512 触发 DNA 损伤反应。AGI-24512 可阻断 MTAP 缺失的癌细胞体外增殖。AGI-24512可用于抗癌研究。
生物活性
AGI-24512 is a potent methionine adenosyltransferase 2α (MAT2A) inhibitor, with an IC 50 of 8 nM. AGI-24512 triggers DNA damage response. AGI-24512 can block proliferation of MTAP-deleted cancer cells in vitro. AGI-24512 can be used for researching anticancer.
性状
Solid
IC50 & Target[1][2]
IC50: 8 nM (MAT2A)
体外研究(In Vitro)
AGI-24512 (0-1 μM; 96 hours) blocks proliferation of MTAP (methylthioadenosine phosphorylase)-deleted HCT116 cancer cells with an IC50 of 100 nM.
AGI-24512 significantly increases in γH2AX-positive cells in MTAP HCT116 cells.
AGI-24512 inhibits PRMT5-mediated SDMA marks with an IC50 of 95 nM in MTAP cells.
AGI-24512 leads to a dose-dependent decrease in SAM (S-adenosylmethionine) levels in the HCT116 MTAP-null cell, with an IC50 of 100 nM. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
AGI-24512 shows poor oral absorption and a short half-life in rats. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件
Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years;In solvent -80°C 6 months
参考文献
[1]. Kalev P, et al. MAT2A Inhibition Blocks the Growth of MTAP-Deleted Cancer Cells by Reducing PRMT5-Dependent mRNA Splicing and Inducing DNA Damage. Cancer Cell. 2021 Feb 8;39(2):209-224.e11.
[2]. Konteatis Z, et al. Discovery of AG-270, a First-in-Class Oral MAT2A Inhibitor for the Treatment of Tumors with Homozygous MTAP Deletion. J Med Chem. 2021 Apr 22;64(8):4430-4449.
溶解度数据
In Vitro: DMSO : 125 mg/mL (312.13 mM; Need ultrasonic)配制储备液
搜索质检报告(COA)

1:一般建议:溶解度为Medlife测试数据,可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异,仅做参考,具体以实验方案为准。

2:储存条件:粉末-20°C一般情况可以保存3年,溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异,请细致阅读产品信息,并辅助参考相关文献描述。

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