| Identification | Back 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 Properties | Back 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 |
| Hazard Information | Back 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. |
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