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NVP-BVU972

In stock
Catalog No.
A8489
C-Met inhibitor,potent and selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$220.00
In stock
5mg
$190.00
In stock
10mg
$260.00
In stock
50mg
$850.00
In stock

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Background

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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt340.38
Cas No.1185763-69-2
FormulaC20H16N6
Solubility≥17mg/mL in DMSO
Chemical Name6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline
SDFDownload SDF
Canonical SMILESCN1C=C(C=N1)C2=NN3C(=NC=C3CC4=CC5=C(C=C4)N=CC=C5)C=C2
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor 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.

Biological Activity

Description NVP-BVU972 is a selective and potent inhibitor of Met with an IC50 value of 14 nM.
Targets Met          
IC50 14 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

NVP-BVU972