| AG-221 (Enasidenib)mutant isocitrate dehydrogenase 2 (IDH2) inhibitor |
Sample solution is provided at 25 µL, 10mM.
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- Purity = 98.98%
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| Cas No. | 1446502-11-9 | SDF | Download SDF |
| 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 | ||
| 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 | ||
| Formula | C19H17F6N7O | M.Wt | 473.37 |
| Solubility | ≥47.3mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
IC50: ~16 nM for IDH2 R140Q mutant
AG-221 (Enasidenib) is a mutant isocitrate dehydrogenase 2 (IDH2) inhibitor.
The somatic mutations of IDH1 and IDH2 are found in patients with acute myeloid leukemia. Leukemia-associated IDH1/2 mutations lead to aberrant accumulation of the oncometabolite 2-hydroxyglutarate (2-HG).
In vitro: AG-221 was found to be able to reduce 2-HG levels by >90%, reverse in-vitro histone and DNA hypermethylation, and induce differentiation in leukemia cell model as well. In addition, a dose dependent proliferative burst of the human specific CD45+ blast cells was observed by the treatment of AG-221, as measured by the expression of CD11b, CD14, CD15 and cell morphology [1].
In vivo: The efficacy of AG-221 in a primary human AML xenograft model with the IDH2 R140Q mutation was studied, and the results showed that AG-221 could reduce 2-HG in the plasma, bone marrow, and urine of engrafted mice potently. In addition, the treatment of AG-221 could also induce a significant and dose dependent survival benefit as demonstrated by that all mice in the high dose treatment of AG-221 survived to the end of study [1].
Clinical trial: A phase 1, multicenter, dose-escalation, safety, PK, PD, and clinical activity study of AG-221 in patients with advanced hematologic malignancies with an IDH2 mutation has been conducted [2].
References:[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
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求有经验的大神指教，我的载体和目的基因连不上，转化不到大肠中，比例为1:3。另外，为啥胶回收后的载体浓度那么低，大约6ng/ul了，影响连接么？
连接酶通常是包括“连接酶”这个字，就如DNA连接酶是将脱氧核糖核酸（DNA）片段连接。其他普遍的名称包括“合成酶”，因为这些酶是用作合成新的分子，或当它们是将二氧化碳加入一个分子时则称为“羧化酶”。
菌体构建时，目的基因连接在T载体上，测序也正确，但是将目的基因还有载体分别双酶切后总是连接不上，将连接后产物跑核酸胶，什么也没有，不知道是什么原因？我的目的基因浓度为9ng/ul,载体回收后的浓度为6ng/ul,是因为浓度太低的原因吗？还有就是连接有目的基因的T载体双酶切后出现了三条带，这个又是什么原因呢？希望得到解答
DNA连接酶主要是连接DNA片段之间的磷酸二酯键最初从原核生物（大肠杆菌）分离得到的.现在生物基因工程主要是从T4噬菌体中分离得到的,
大家有用过Invitrogen的T4连接酶吗？说明书上是23－26度连接，一般的连接酶不都是16度吗？应该用多少度呢？另外，说明书上还说连接后为了达到更好的转化效率，应将连接反应液至少稀释5倍再转化，是这样吗？谢谢大家帮忙啊
DNA连接酶:可以连接被限制酶切割开磷酸二酯键
产生这一现象的原因在于 DNA合成酶只能沿5'-3'的方向合成DNA 而DNA本身的两条链又是反向分布的 所以就造成了只有一条链合成可以连续地进行下去（以它为模板的子链生成方向正好是DNA聚合酶可以直接提供的） 而后随链要盘绕成回环 反扭过来 才能合成
再合成起始的时候 DNA聚合酶是需要一段RNA引物的 在原核生物中这一引物是由dnaQ(一种酶)在已解旋的单链5'端合成，真核生物中也有对应的酶 由于后随链的合成不连续 所以每个片段都要有引物 在DNA合成结束的时候 这些引物要被切除 因而留下缺口 这时又要特定的酶去填补缺口（比如 大肠杆菌中的DNA聚合酶I）可是填补序列和周围序列间会有缺刻 也就是说他们交界处的3'-5'磷酸二脂键是断开的 这时需要DNA连接酶发挥作用 将其连好
所以 后随链上的缺刻多 还真够DNA连接酶忙一阵的 前导链上只有一开始有RNA引物 因此 最后也基本只有这个地方会用到连接酶
