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NVP-BVU972
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
NVP-BVU972图片
CAS NO:1185763-69-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
NVP-BVU972 是一种选择性和有效的 Met 抑制剂,IC50 为 14 nM。 NVP-BVU972 还对具有耐药突变的 Met 表现出良好的抗增殖活性并抑制磷酸化。 NVP-BVU972可用于癌症研究。
Cas No.1185763-69-2
别名6-[[6-(1-甲基-1H-吡唑-4-基)咪唑并[1,2-B]哒嗪-3-基]甲基]喹啉
化学名6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline
Canonical SMILESCN1C=C(C=N1)C2=NN3C(=NC=C3CC4=CC5=C(C=C4)N=CC=C5)C=C2
分子式C20H16N6
分子量340.38
溶解度≥ 17mg/mL in DMSO
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

NVP-BVU972 is a selective and potent inhibitor of c-Met with IC50 of 14 nM. Besides, NVP-BVU972 displays IC50 values more than 1000 nM in other kinases such as the most closely related kinase recepteur d'origine nantais (RON).

c-Met, also known as hepatocyte growth factor receptor, is a receptor tyrosine kinase that can be activated by hepatocyte growth factor/scatter factor (HGF/SF). It is a membrane protein which plays an essential role in embryonic development and wound healing.

In the EBC-1, GTL-16, and MKN-45 human cancer cells, NVP-BVU972 potently inhibits the cell proliferation with IC50 values of 82, 66 and 32 nM, respectively. Additionally, NVP-BVU972 treatment leads to the inhibition of the growth of the transformed mouse BaF3 cells containing TPR-MET kinase fusions with IC50 of 104 nM 1.

In human sample, NVP-BVU972 treatment on cells expressing wild-type TPR-MET resulted in a dose-dependent reduction in TPR-MET phosphorylation. Y1230H, D1228A, F1200I and L1195V mutations abrogate the TPR-MET phosphorylation inhibition effect of NVP-BVU972 in BaF3 TPR-MET1.

Reference:
1.   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.