2. Epigenetics Metabolic Enzyme/Protease
  3. Methionine Adenosyltransferase (MAT)
  4. AGI-25696

AGI-25696 是一种具有口服活性的乙硫氨酸腺苷转移酶 2A (MAT2A) 抑制剂，其 IC50 为 97 nM。AGI-25696 可降低癌细胞内的 SAM 水平。AGI-25696 可抑制携带皮下 KP4 MTAP 缺失胰腺异种移植物的小鼠的肿瘤生长。AGI-25696 可用于 mtap 缺失胰腺癌的研究。

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AGI-25696

AGI-25696 Chemical Structure

CAS No. : 2201065-84-9

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AGI-25696 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

AGI-25696 is an orally active ethionine adenosyltransferase 2A (MAT2A) inhibitor with an IC50 of 97 nM. AGI-25696 reduces intracellular SAM levels in cancer cells. AGI-25696 inhibits tumor growth in mice bearing subcutaneous KP4 MTAP-null pancreatic xenografts. AGI-25696 can be used for the research of mtap-deleted pancreatic cancer[1].

IC50 & Target[1]

MAT2A

97 nM (IC50)

体外研究
(In Vitro)

AGI-25696 可强效抑制纯化的重组 MAT2A 同源二聚体，其 IC50 为 97 nM[1]。
AGI-25696 (72 h) 可剂量依赖性降低 HCT116 MTAP 缺陷细胞内的 SAM 水平，其 IC50 为 150 nM，72 h 后最大抑制率达 84%[1]。

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

AGI-25696 相关抗体:
体内研究
(In Vivo)

AGI-25696 (300 mg/kg；口服；每日 1 次；连续 33 天) 在皮下接种 KP4 MTAP 缺失型胰腺异种移植物的小鼠中实现了 67.8% 的肿瘤生长抑制率，且未观察到体重下降[1]。

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

Animal Model: Mice bearing subcutaneous KP4 MTAP-null
xenografts[1]
Dosage: 300 mg/kg
Administration: p.o.; once daily; 33 days
Result: Achieved a tumor growth inhibition (TGI) of 67.8% relative to vehicle-treated controls.
Caused no adverse effects on mouse body weight during the 33-day study.
分子量

428.48

Formula

C28H20N4O
CAS 号
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

AGI-25696 相关分类

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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.

Keywords:

AGI-256962201065-84-9AGI25696AGI 25696Methionine Adenosyltransferase (MAT)S-adenosylmethionine Synthetasemtap-deleted pancreatic cancerhuman liver microsomesMAT2Apancreatic KP4 MTAP-null xenograft tumorsHCT116 MTAP-null cellsSAMMTAP-null cancer cellsInhibitorinhibitorinhibit

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