NVP-BVU972
![mRNA synthesis](/media/diy/images/page/figure1-mrna.png)
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
![Tyramine Signal Amplification (TSA)](/media/diy/images/page/figure2-01.png)
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
![screening library](/media/diy/images/page/figure3-01.png)
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
![Cell Counting Kit-8 (CCK-8)](/media/diy/images/page/CCK-8.jpg)
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
![SYBR Safe DNA Gel Stain](/media/diy/images/page/SYBR Safe DNA Gel Stain.png)
SYBR Safe DNA Gel Stain
Safe and sensitive stain for visualization of DNA or RNA in agarose or acrylamide gels.
![Inhibitor Cocktails](/media/diy/images/page/Inhibitor Cocktails.jpg)
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
NVP-BVU972是高效选择性c-Met抑制剂,其IC50值为14 nM。NVP-BVU972对其它激酶的IC50值超过1000 nM,如最密切相关的激酶受体RON。
c-Met也称为肝细胞生长因子受体,是一种受体酪氨酸激酶,能被肝细胞生长因子/散因子(HGF/SF)激活。其作为一种膜蛋白在胚胎发育和伤口愈合中起重要作用。
在EBC-1、GTL-16和MKN-45人肿瘤细胞中,NVP-BVU972高效抑制细胞增殖,其IC50值分别为82、66和32 nM。此外,NVP-BVU972处理包含融合TPR-MET激酶的转化小鼠BaF3细胞会抑制细胞生长[1]。
在人样本中,NVP-BVU972处理表达野生型TPR-MET的细胞会以剂量依赖的方式减少TPR-MET磷酸化。在BaF3 TPR-MET细胞中,Y1230H、D1228A、F1200I和L1195V突变则会消除NVP-BVU972抑制TPR-MET磷酸化的能力。
参考文献:
Tiedt R, Degenkolbe E, Furet P, et al. A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. Cancer research. 2011;71(15):5255-5264.
Physical Appearance | A solid |
Storage | Store at -20°C |
M.Wt | 340.38 |
Cas No. | 1185763-69-2 |
Formula | C20H16N6 |
Solubility | insoluble in H2O; ≥17 mg/mL in DMSO; ≥25.15 mg/mL in EtOH |
Chemical Name | 6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline |
SDF | Download SDF |
Canonical SMILES | CN1C=C(C=N1)C2=NN3C(=NC=C3CC4=CC5=C(C=C4)N=CC=C5)C=C2 |
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。 |
Description | NVP-BVU972是高效选择性c-Met抑制剂,其IC50值为14 nM。 | |||||
靶点 | Met | |||||
IC50 | 14 nM |
化学结构
![NVP-BVU972](http://www.apexbt.com//media/diy/images/struct/A8489.png)