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ChemicalBook--->CAS DataBase List--->1185763-69-2

1185763-69-2

1185763-69-2 Structure

1185763-69-2 Structure
IdentificationBack Directory
[Name]

NVP-BVU 972
[CAS]

1185763-69-2
[Synonyms]

CS-529
NVP-BVU972
NVP-BVU 972
NVP-BVU972, >=98%
NVP-BVU 972 USP/EP/BP
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
[EINECS(EC#)]

200-258-5
[Molecular Formula]

C20H16N6
[MDL Number]

MFCD22420820
[MOL File]

1185763-69-2.mol
[Molecular Weight]

340.38
Chemical PropertiesBack Directory
[density ]

1.35
[storage temp. ]

Store at -20°C
[solubility ]

insoluble in H2O; ≥17 mg/mL in DMSO; ≥25.15 mg/mL in EtOH
[form ]

solid
[pka]

4.92±0.10(Predicted)
[color ]

White to off-white
Safety DataBack Directory
[Symbol(GHS) ]


GHS07
[Signal word ]

Warning
[Hazard statements ]

H317-H319
[Precautionary statements ]

P280-P305+P351+P338
Hazard InformationBack Directory
[Uses]

NVP-BVU972 exhibits strong inhibition towards MET kinase but displays low inhibition against other kinases including the most closely related kinase RON.
[Biological Activity]

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.
[target]

Met
[References]

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.
Spectrum DetailBack Directory
[Spectrum Detail]

NVP-BVU 972(1185763-69-2)1HNMR
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