AMG 337 |
| Catalog No.GC15655 |
MET inhibitor
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1173699-31-4
Sample solution is provided at 25 µL, 10mM.
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IC50: < 5 nM in enzymatic assays
AMG 337 is a MET inhibitor.
MET receptor with its ligand can promote cell survival, proliferation, and invasion. The activation of MET signaling is a common regulator of various human cancer types, and thus, inhibition of MET signaling is an promising therapeutic opportunity for the treatment of cancer.
In vitro: AMG 337 could effectively inhibit MET kinase activity, and AMG 337 also showed great selectivity for MET when tested against a panel of over 400 protein as well as lipid kinases. In addition, AMG 337 was found to inhibit HGF-dependent MET phosphorylation. Furthermore, AMG 337 could only affect the viability of two gastric cancer cell lines with amplification of the MET gene. The IC50 values of AMG 337 for the two sensitive cell lines was less than 50 nM, whereas over 10 μM in all other tested cell lines [1].
In vivo: In anima study, it was found that the oral administration of AMG 337 led to the dose-dependent anti-tumor efficacy in MET amplified gastric cancer xenograft models, which was quite consistent with the PD modulation of MET signaling [1].
Clinical trial: A phase 1 clinical study is currently investigating the safety, tolerability and PK of AMG 337 in patients with solid tumors [2].
References:
[1] Paul E. Hughes, et al. AMG 337, a novel, potent and selective MET kinase inhibitor, has robust growth inhibitory activity in MET-dependent cancer models. Cancer Res October 1, 2014 74; 728
[2] https://clinicaltrials. gov/ct2/show/NCT01253707 term=AMG+337&rank=1
| Cas No. | 1173699-31-4 | SDF | |
| Chemical Name | (R)-6-(1-(8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridin-3-yl)ethyl)-3-(2-methoxyethoxy)-1,6-naphthyridin-5(6H)-one | ||
| Canonical SMILES | CN1N=CC(C2=CN3C([C@@H](C)N4C=CC(N=CC(OCCOC)=C5)=C5C4=O)=NN=C3C(F)=C2)=C1 | ||
| Formula | C23H22FN7O3 | M.Wt | 463.46 |
| Solubility | ≥ 46.3mg/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. |
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| 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 | 2.1577 mL | 10.7884 mL | 21.5768 mL |
| 5 mM | 0.4315 mL | 2.1577 mL | 4.3154 mL |
| 10 mM | 0.2158 mL | 1.0788 mL | 2.1577 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 13 reference(s) in Google Scholar.)
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