NVP-BVU972 Inhibitor CAS No. 1185763-69-2

Cat. No.	Name	Size	Price
KI0123	NVP-BVU972	5 mg	$400
	NVP-BVU972	10 mg	$592
	NVP-BVU972	50 mg	$1600
	NVP-BVU972	200 mg	$3952

Chemical Characteristic

Product Name	NVP-BVU972
CAS No.	1185763-69-2
Molecular Weight	340.38
Formula	C₂₀H₁₆N₆
Chemical Name	6-[[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline
Smiles	n1cccc2cc(ccc12)Cc1n2c(ccc(n2)c2cnn(c2)C)nc1
Chemical Structure

Biological activities

NVP-BVU972 is a selective and potent MET kinase inhibitor with IC50 of 14 nM. NVP-BVU972 displays IC50 values greater than 1000 nM in other kinases including the most closely related kinase recepteur d'origine nantais (RON). NVP-BVU972 also inhibits MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 and 22 nM, respectively. In MET-amplified GTL-16, EBC-1, and MKN-45 human cancer cells, NVP-BVU972 potently prevents the cell proliferation with IC50 values of 66, 82 and 32 nM, respectively. NVP-BVU972 potently prevents the growth of the transformed mouse BaF3 cells containing TPR-MET kinase fusions with IC50 of 104 nM. In the NVP-BVU972 resistance screen in BaF3 TPR-MET cells, the percentage of resistance mutations Y1230 and D1228 is 88.2% and 9.4, respectively. The overall yield of clones (Y1230, D1228, V1155 and F1200 mutations) decreases significantly at the 2 highest concentrations of NVP-BVU972 (4.8 and 9.6 µM). In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations cause dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell proliferation assays. A dose-dependent reduction in TPR-MET phosphorylation is observed when applying NVP-BVU972 to cells expressing wild-type TPR-MET. Y1230H, D1228A, F1200I and L1195V mutations abrogate the TPR-MET phosphorylation inhibition effect of NVP-BVU972 in BaF3 TPR-MET clones.^[1]

Protocols

NVP-BVU972 is dissolved and diluted in DMSO and assayed in quadruplicate. ^[1]

References

[1] Tiedt R, 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 Res. 2011, 71(15): 5255-5264.

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