NVP-BVU972 |
| カタログ番号GC16972 |
NVP-BVU972 は、選択的で強力な Met 阻害剤であり、IC50 は 14 nM です。 NVP-BVU972 は、薬剤耐性変異を持つ Met に対しても優れた抗増殖活性を示し、リン酸化を阻害します。 NVP-BVU972 は、がんの研究に使用できます。
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1185763-69-2
Sample solution is provided at 25 µL, 10mM.
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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.
Reference:
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.
| Cas No. | 1185763-69-2 | SDF | |
| Chemical Name | 6-[[6-(1-methylpyrazol-4-yl)imidazo[1,2-b]pyridazin-3-yl]methyl]quinoline | ||
| Canonical SMILES | CN1C=C(C=N1)C2=NN3C(=NC=C3CC4=CC5=C(C=C4)N=CC=C5)C=C2 | ||
| Formula | C20H16N6 | M.Wt | 340.38 |
| 溶解度 | ≥ 17mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.9379 mL | 14.6895 mL | 29.3789 mL |
| 5 mM | 0.5876 mL | 2.9379 mL | 5.8758 mL |
| 10 mM | 0.2938 mL | 1.4689 mL | 2.9379 mL |
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)
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