计算溶液所需的质量、体积或浓度。
AG-270
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。
概述
AG-270 is an allosteric, noncompetitive, first-in-class, reversible and orally active MAT2A inhibitor, with an IC 50 of 14 nM
In Vitro
AG-270 demonstrates potent reduction in levels of intracellular SAM , as well as MTAP-–selective antiproliferative activity in the HCT116 MTAP isogenic cell model in vitro. AG-270 exhibits an IC 50 of 20 nM in HCT116 MTAP- cell SAM at 72 h. MAT2A is a key enzyme in the methionine salvage pathway, responsible for generating the universal methyl donor, S-adenosylmethionine (SAM). MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
AG-270 shows excellent microsomal, hepatocyte, and in vivo metabolic stability across species (human, mouse, rat, dog, and monkey). AG-270 exhibits T1/2 values of 5.9 h, 4.2 h, 4.8 h and 21.3 h in mouse, rat, monkey and dog, respectively . AG-270 (200 mg/kg, orally, q.d. for 38 days) results in dose-dependent reduction in tumor SAM levels and tumor growth of KP4 MTAP- xenografts and is well tolerated, with mean body weight loss <5% . Combining AG-270 with taxanes and gemcitabine yielded additive-tosynergistic antitumor activity, with the docetaxel combination yielding 50% complete tumor regressions in select models; combination benefits are observed in PDX models derived from esophageal, NSCLC, and pancreatic cancers. MCE has not independently confirmed the accuracy of these methods. They are for reference only. Animal Model: Pancreatic KP4 MTAP - xenograft mouse model . Dosage: 10-200 mg/kg. Administration: Orally, q.d. for 38 days. Result: Led to dose-dependent reductions in tumor SAM levels and tumor growth of KP4 MTAP- xenografts (TGI = 36% (10 mg/kg), 48% (30 mg/kg), 66% (100 mg/kg), 67% (200 mg/kg).
IC50& Target:IC50: 14 nM (MAT2A)
规格
规格或纯度
Moligand™, 10mM in DMSO
英文名称
AG-270
生化机理
AG-270 是一种异构、非竞争性、一流、可逆和口服活性 MAT2A 抑制剂，其 IC 50 为 14 nM。
储存条件
-80℃储存
运输条件
特低温运输
名称和识别符
分子类型
小分子
Isomeric SMILES
COC1=CC=C(C=C1)C2=C(N=C3C(=C(NN3C2=O)C4=CC=CC=C4)C5=CCCCC5)NC6=CC=CC=N6
关联CAS
PubChem CID
分子量
489.57
技术文档
高级数据
安全和危险性（GHS）
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
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| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 J2610916 |
分析证书 | A655557 |
技术文档和文章
溶液计算器
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