NVP-BVU972
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.
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 |