NVP-BVU972|cas 1185763-69-2

Cas No.:	1185763-69-2
Chemical Name:	NVP-BVU972
Synonyms:	NVP-BVU972;6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline;6-[6-(1-methyl-1H-pyrazol-4-yl)-imidazo[1,2-b]pyridazin-3-ylmethyl]quinoline;3qti;6-((6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl)methyl)quinoline;BVU972;CS-0967;NVPBVU972;C20H16N6;6-{[6-(1-Methyl-1h-Pyrazol-4-Yl)imidazo[1,2-B]pyridazin-3-Yl]methyl}quinoline;RNCNPRCUHHDYPC-UHFFFAOYSA-N;NVP BVU972;MLS006010964;AOB2279;HMS3656L04;BCP03600;BDBM50146169;2607AH;s2761;BCP9000466;AK474020;BC;NVP-BVU-972;SCHEMBL1659100;SW219959-1;CHEMBL1738731;NVP-BVU 972;NCGC00346689-01;AS-56284;CCG-267923;BVU-972;AKOS026750599;AC-35941;SMR004702768;EX-A2116;DTXSID40657890;1185763-69-2;6-{[6-(1-METHYLPYRAZOL-4-YL)IMIDAZO[1,2-B]PYRIDAZIN-3-YL]METHYL}QUINOLINE;GLXC-04408;DA-66277;NCGC00346689-06;Q27454048;NCGC00346689-02;C71592;BRD-K77943374-001-02-8;6-[6-(1-methyl-1h-pyrazol-4-yl)-imidazo[1,2-b]pyridazin-3-ylmethyl]-quinoline;HY-15456;SDCCGSBI-0654467.P001;BCP0726000188
SMILES:	N12C(C([H])=C([H])C(C3C([H])=NN(C([H])([H])[H])C=3[H])=N1)=NC([H])=C2C([H])([H])C1C([H])=C([H])C2=C(C([H])=C([H])C([H])=N2)C=1[H]
Formula:	C₂₀H₁₆N₆
M.Wt:	340.3812
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.NVP-BVU972 potently inhibits MET kinase but displays low inhibition against other kinases including the most closely related kinase RON with IC50 values of more than 1000 nM. NVP-BVU972 also suppresses constitutive MET phosphorylation in GTL-16 cells or HGF-stimulated MET phosphorylation in A549 cells with IC50 values of 7.3 nM and 22 nM, respectively. NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC50 values of 66 nM, 82 nM and 32 nM, respectively. In line with their high frequency in the NVP-BVU972 screen, Y1230 and D1228 mutations give rise to dramatic shifts in the measured IC50 values for NVP-BVU972 in BaF3 cell line. Resistance triggered by V1155L is more limited to NVP-BVU972. A dose-dependent reduction in TPR-MET phosphorylation when applying NVP-BVU972 to BaF3 cells expressing wild-type TPR-MET. Both Y1230H and D1228A mutations abrogated the effect of NVP-BVU972 but not AMG 458. However, F1200I and L1195V interferes with the potency of NVP-BVU972 to prevent TPR-MET phosphorylation.

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