1185763-69-2

Name	NVP-BVU972
Synonyms	CS-529 NVP-BVU972 NVP-BVU 972 6-[[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline Quinoline, 6-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]- 6-[[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline NVP-BVU972
CAS	1185763-69-2
EINECS	200-258-5

Molecular Formula	C20H16N6
Molar Mass	340.38
Density	1.35
pKa	4.92±0.10(Predicted)
Storage Condition	-20℃
In vitro study	NVP-BVU972 efficient inhibition of MET kinase, while inhibition of other kinases, including the most closely related kinase RON, was very low, with an IC50 above 1000 nM. NVP-BVU972, it inhibited constitutive MET phosphorylation in GTL-16 cells, and inhibited HGF-stimulated MET phosphorylation in A549 cells, with IC50 of 7.3 and 22 nM, respectively. Cell lines that potently inhibited the proliferation of the MET gene by NVP-BVU972, GTL-16 and MKN-45 grew at IC50 of 66, 82 and 32 nM, respectively. NVP-BVU972 acting on BaF3 cells, Y1230 and D1228 mutations cause a dramatic change in the measured IC50. The resistance induced by V1155L is limited by NVP-BVU972. The effect of NVP-BVU972 on BaF3 cells expressing wild-type TPR-MET decreased phosphorylation by TPR-MET in a dose-dependent manner. Y1230H and D1228A mutations abrogate the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interference NVP-BVU972 inhibited TPR-MET phosphorylation.

Last Update：2024-01-02 23:10:35

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CAS: 1185763-69-2
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409

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1185763-69-2

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