NVP-BVU972
Modify Date: 2024-01-02 22:13:18
NVP-BVU972 structure
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Common Name | NVP-BVU972 | ||
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| CAS Number | 1185763-69-2 | Molecular Weight | 340.381 | |
| Density | 1.4±0.1 g/cm3 | Boiling Point | N/A | |
| Molecular Formula | C20H16N6 | Melting Point | N/A | |
| MSDS | N/A | Flash Point | N/A | |
Use of NVP-BVU972NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.IC50 value: 14 nM [1]Target: MetNVP-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. |
| Name | 6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline |
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| Synonym | More Synonyms |
| Description | NVP-BVU972 is a selective and potent Met inhibitor (IC50 = 14 nM). Antitumor agents.IC50 value: 14 nM [1]Target: MetNVP-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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| Related Catalog | |
| References |
| Density | 1.4±0.1 g/cm3 |
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| Molecular Formula | C20H16N6 |
| Molecular Weight | 340.381 |
| Exact Mass | 340.143646 |
| PSA | 60.90000 |
| LogP | 2.12 |
| Index of Refraction | 1.745 |
| Storage condition | -20℃ |
| Hazard Codes | N |
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NVP-BVU972 CAS#:1185763-69-2 |
| Literature: WO2009/106577 A1, ; Page/Page column 77-78 ; |
![(rac)-[6-(1-methyl-1H-pyrazol-4-yl)-imidazo[1,2-b]pyridazin-3-yl]-quinolin-6-yl-methanol structure](https://image.chemsrc.com/caspic/100/1185763-68-1.png)
| Precursor 1 | |
|---|---|
| DownStream 0 | |
| BVU972 |
| cc-601 |
| CS-0967 |
| 6-((6-(1-methyl-1H-pyrazol-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-yl]methyl}quinoline |
| 3qti |
| Quinoline, 6-[[6-(1-methyl-1H-pyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]- |
| NVPBVU972 |
| NVP-BVU972 |