AG-221 (Enasidenib)
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.
作用于IDH2 R140Q突变体，IC50约为16 nM。
AG-221（Enasidenib）是突变异柠檬酸脱氢酶2（IDH2）抑制剂。
在急性骨髓性白血病患者中发现IDH1和IDH2的体细胞突变。白血病相关的IDH1 / 2突变导致代谢产物2-羟基戊二酸（2-HG）的异常积累。
体外：研究发现AG-221能够将2-HG水平降低超过90％，逆转体外组蛋白和DNA超甲基化，并诱导白血病细胞模型中的分化。此外，通过测量CD11b、CD14、CD15的表达和细胞形态学，观察到AG-221治疗引起人特异性CD45+胚细胞剂量依赖性的增殖爆发[1]。
体内：研究AG-221在具有IDH2 R140Q突变的原发性人AML异种移植物模型中的功效，结果显示AG-221可有效降低移植小鼠的血浆、骨髓和尿中的2-HG。此外，AG-221的高剂量治疗中所有小鼠存活至研究结束，表明AG-221治疗还可以诱导显著的和剂量依赖性的存活改善[1]。
临床试验：已经在具有IDH2突变的晚期血液恶性肿瘤患者中进行AG-221的1期、多中心、剂量递增、安全性、PK、PD和临床活性研究[2]。
参考文献：
[1] Kate Ellwood-Yen, Fang Wang, Jeremy Travins, Yue Chen, Hua Yang, Kim Straley, Sung Choe, Marion Dorsch, Sam Agresta, David Schenkein, Scott Biller, Michael Su. AG-221 offers a survival advantage in a primary human IDH2 mutant AML xenograft model. [abstract]. In: Proceedings of the 105th Annual Meeting of the American Association for Cancer Research; 2014 Apr 5-9; San Diego, CA. Philadelphia (PA): AACR; Cancer Res 2014;74(19 Suppl):Abstract nr 3116. doi:10.1158/1538-7445.AM2014-3116
[2] https://clinicaltrials. gov/ct2/show/NCT02577406term=Enasidenib&rank=1
| Physical Appearance | A solid |
| Storage | Store at -20°C |
| M.Wt | 473.37 |
| Cas No. | 1446502-11-9 |
| Formula | C19H17F6N7O |
| Solubility | ≥47.3 mg/mL in DMSO; insoluble in H2O; ≥22.9 mg/mL in EtOH |
| Chemical Name | 2-methyl-1-((4-(6-(trifluoromethyl)pyridin-2-yl)-6-((2-(trifluoromethyl)pyridin-4-yl)amino)-1,3,5-triazin-2-yl)amino)propan-2-ol |
| SDF | Download SDF |
| Canonical SMILES | CC(O)(C)CNC1=NC(C2=NC(C(F)(F)F)=CC=C2)=NC(NC3=CC(C(F)(F)F)=NC=C3)=N1 |
| 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
