AG-120
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
IC50低于100 nM。
AG-120是一种IDH1抑制剂。
异柠檬酸脱氢酶（IDH）是一种代谢酶，相互转化异柠檬酸和α-酮戊二酸（α-KG），但IDH1和IDH2的癌症相关突变赋予新生体活性，使得α-KG还原为代谢物2-HG。
体外：用AG-120处理表达突变IDH1的TF-1细胞或原发性人AML患者样品，结果显示在TF-1 IDH1-R132H细胞中，AG-120能够降低细胞内2-HG水平，抑制生长因子非依赖性增殖并恢复促红细胞生成素诱导的分化[1]。
离体：先前的离体研究表明，在原发性人胚细胞中用AG-120对突变IDH1酶的药理学抑制导致有效降低细胞内2-HG水平并诱导骨髓分化[1]。
临床试验：在I期临床试验中，62名具有晚期IDH1突变阳性实体瘤的患者每天一次口服单剂AG-120。结果显示，11例IDH1突变阳性软骨肉瘤患者中有7例病情稳定; 20例IDH1突变阳性IHCC患者中有1例部分缓解，11例有SD;4例其他IDH1突变阳性实体瘤患者中一例有SD [2]。
参考文献：
[1] EricaHansen et al. AG-120, an Oral, Selective, First-in-Class, Potent Inhibitor of Mutant IDH1, Reduces Intracellular 2HG and Induces Cellular Differentiation in TF-1 R132H Cells and Primary Human IDH1 Mutant AML Patient Samples TreatedEx Vivo. Blood2014124:3734.
[2] http://www. aacr.org/Newsroom/Pages/News-Release-Detail.aspxItemID=789#.WLAUOm997IU
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 582.96 |
| Cas No. | 1448347-49-6 |
| Formula | C28H22ClF3N6O3 |
| Solubility | ≥58.3 mg/mL in DMSO; insoluble in H2O; ≥63.3 mg/mL in EtOH |
| Chemical Name | (S)-N-((S)-1-(2-chlorophenyl)-2-((3,3-difluorocyclobutyl)amino)-2-oxoethyl)-1-(4-cyanopyridin-2-yl)-N-(5-fluoropyridin-3-yl)-5-oxopyrrolidine-2-carboxamide |
| SDF | Download SDF |
| Canonical SMILES | O=C([C@H](CC1)N(C2=NC=CC(C#N)=C2)C1=O)N([C@@H](C3=CC=CC=C3Cl)C(NC4CC(F)(F)C4)=O)C5=CC(F)=CN=C5 |
| 运输条件 | 蓝冰运输或根据您的需求运输。 |
| 一般建议 | 不同厂家不同批次产品溶解度各有差异，仅做参考。若实验所需浓度过大至产品溶解极限，请添加助溶剂助溶或自行调整浓度。溶液形式一般不宜长期储存，请尽快用完。 |
质量控制和MSDS
- 批次:
化学结构
