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| NVP-BVU 972 Basic information |
| Product Name: | NVP-BVU 972 | | Synonyms: | 6-[[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline NVP-BVU972;NVP-BVU 972;NVP-BVU972;6-[[6-(1-Methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline;NVP-BVU972, >=98%;NVP-BVU972;NVP-BVU 972;CS-529;Quinoline, 6-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]- | | CAS: | 1185763-69-2 | | MF: | C20H16N6 | | MW: | 340.38 | | EINECS: | 200-258-5 | | Product Categories: | Inhibitors | | Mol File: | 1185763-69-2.mol |
| NVP-BVU 972 Chemical Properties |
| density | 1.35 | | solubility | insoluble in H2O; ≥17 mg/mL in DMSO; ≥25.15 mg/mL in EtOH | | form | solid | | pka | 4.92±0.10(Predicted) |
| NVP-BVU 972 Usage And Synthesis |
| 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. | | 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. |
| NVP-BVU 972 Preparation Products And Raw materials |
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