
Molecular Weight: | 410.39 |
Formula: | C18H21F3N6O2 |
Purity: | ≥98% |
CAS#: | 944396-07-0 |
Solubility: | DMSO up to 100 mM |
Chemical Name: | 5-(2,6-dimorpholinopyrimidin-4-yl)-4-(trifluoromethyl)pyridin-2-amine |
Storage: | Powder:4oC 1 year. DMSO:4oC3 month;-20oC 1 year. |
Biological Activity:BKM120 (NVP-BKM120) is a potent and selective, orally available pan-class I phosphatidylinositol 3-kinase (PI3K) inhibitor. It inhibits all four class-I PI3K isoforms in biochemical assays with IC50 ~50-250 nM, but exhibits selectivity of >100 folds against other protein kinases. It is also active against the most common somatic PI3Ka mutations but does not significantly inhibit the related class-III (Vps34) and class-IV (mTOR, DNA-PK) PI3K kinases. BKM120 has shown to significantly inhibit cell growth and induce apoptosis in a variety of tumor cell lines as well as in animal models. Consistent with its mechanism of action, NVP-BKM120 decreases the cellular levels of p-Akt in relevant models, as well as modulates downstream effectors in a concentration dependent and pathway-specific manner.
How to Use:
- In vitro: BKM120 was typically used at 1 µM in vitro and cellular assays.
- In vivo: BKM120 was formulated in NMP/PEG300 (10/90, v/v) and orally dosed to mice at 10 mg/kg once per day.
Reference:
- 1. Maira SM, et al. Identification and characterization of NVP-BKM120, an orally available pan-class I PI3-kinase inhibitor. (2012) Mol Cancer Ther. 11(2):317-28.
- 2. Koul D, et al. Antitumor activity of NVP-BKM120--a selective pan class I PI3 kinase inhibitor showed differential forms of cell death based on p53 status of glioma cells. (2012) Clin Cancer Res. 18(1):184-95.
- 3. Park E, et al. NVP-BKM120, a novel PI3K inhibitor, shows synergism with a STAT3 inhibitor in human gastric cancer cells harboring KRAS mutations. (2012) Int J Oncol. 40(4):1259-66
- 4. Brachmann SM, et al. Characterization of the mechanism of action of the pan class I PI3K inhibitor NVP-BKM120 across a broad range of concentrations. (2012) Mol Cancer Ther.
- 5.Ren H, et al. The combination of RAD001 and NVP-BKM120 synergistically inhibits the growth of lung cancer in vitro and in vivo.
BKM120_spec.pdf
BKM120_MSDS.pdf
Products are for research use only. Not for human use.
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RMgX + RX = R-R + MgX2.
这个反应需要的能量比生成格氏试剂的高,
因此降低反应温度是第一个选择。
其次, 增加镁得摩尔比, 让 RX与镁有更多机会反应, 而不是与RMgX。
第三, 降低RX的浓度, 即用更多的溶剂, 因为溶剂和格氏试剂有很显著的溶剂络合。
第四, 缓慢滴加RX., 即降低RX.在反应体系的浓度。
第五, 增加搅拌速率, 即, 让RX.与镁有更好的接触。
、
Cell-Based ELISA
的优点:
Cell-Based ELISA
(基于细胞的
ELISA
)是一种全新的
ELISA
技术,有两个最突出的优点:
1.1
不需要抽提蛋白、包被微孔板:细胞直接在微孔板里培养,待检测的时候,将细胞固定在微孔板上并
进行通透处理即可。这样就避免了抽提蛋白时,由于客观和主观上引起样品的损失而导致实验结果在一定
程度上偏离了实际情况。
同时不用包被微孔板,
简化了实验流程,
有助于提高效率。
科研人员在一个
96
孔
酶联板上,便能检测目标细胞蛋白经刺激或抑制作用后的表现。由于省去抽提蛋白和裂解细胞的步骤,样
本的损失也能降到最低,比起其他普通的
ELISA
测定方法,这项全新的
ELISA
技术能更快速、更方便
地一次检测大量的细胞内蛋白。
1.2
可同时检测两种不同蛋白:
封闭后加入两种抗不同蛋白且来源于不同宿主的一抗,
然后再加入不同的
二抗,加入两种荧光底物,检测两个波长。同时检测两种蛋白的好处是显而易见的,可以减少工作量,此
外还可以满足一些特殊的实验需要,例如,需要测定某个蛋白的磷酸化比例,就需要测定磷酸化蛋白的数
量和总蛋白的数量,这两个测定在同一次实验进行,有助于消除实验误差,得到更为精确的实验结果。
2
、
Cell-Based ELISA
的两种技术:
某些公司发展了双通道
Cell-Based ELISA
技术;
双通道与单通道
Cell-based ELISA
比较:
双通道
cell-based ELISA
,顾名思义,即一次可以同时检测两种目的蛋白,
R&D Systems
提供的
Cell-based ELISA
就是双通道
cell-based ELISA
,原理略:(需要荧光检测方式和相应仪器);
单通道
cell-based ELISA
,即一次只能检测一种目的蛋白,他和普通
ELISA
的主要区别在于样品处理过
程
3
、
cell-based ELISA
的应用:
该产品,最多发展起来的是用于检测磷酸化和非磷酸化蛋白的相对含量;
4
、有
cell-based ELISA
产品的公司:目前,多家
elisa
产品提供
商均
提供
cell
based
elisa
试剂盒,
如
Rnd
systems
,
raybiotech
,
ebioscience
,
millipore
等公司;
5
、如何自己进行
cell based elisa
实验?
事实上,根据单通道的
cell based elisa
原理,可以自己建立
cell based elisa
实验系统;
细胞加入培养板中;
加入刺激物或者抑制剂进行培养;
对细胞进行固定或者封闭;
加入第一抗体;
加入
HRP
结合的二抗(二抗的选择,同
western blot
);
加入底物进行显色;
天然产物,大多都有颜色,
存在干扰,多数情况下需要做样品的阴性对照,
尽量能用荧光的方法,
之前我们做过,将两个试剂盒的方法合并后,做的,
效果还可以
1. 姜黄素是一个典型的HAT抑制剂。
2. 针对P300: 在大约10年前,Cole和他的同事设计出了一种p300/CBP抑制剂,发表在nature杂志上。
希望能帮到你,望采纳!

