AMG-458 (Synonyms: AMG 458; AMG458) |
| Catalog No.GC11481 |
AMG-458은 인간 및 마우스 c-Met에 대해 각각 1.2nM 및 2.0nM의 Ki 값을 갖는 강력하고 선택적이며 경구 생체이용 가능한 c-Met 억제제입니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 913376-83-7
Sample solution is provided at 25 µL, 10mM.
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AMG-458 is a potent and selective inhibitor of human and mouse c-Met with IC50 value of 1.2 nM and 2.0 nM respectively.
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.
Recent study investigated the effect of AMG-456 treatment on cell radiosensitizing response. The results showed that AMG-458 treatment enhanced radiosensitivity in H441 with higher levels of c-Met but not in A549 with lower expression of c-Met [1].
This component was also used in an animal model to study the role of c-Met in the development of tumor. For instance, orally administration of AMG-456 resulted in significant inhibition of tumor growth in /TPR-Met and U-87 MG xenograft models without any adverse effect on body weight [2].
References:
1. Li B, Torossian A, Sun Y, Du R, Dicker AP, Lu B. Higher levels of c-Met expression and phosphorylation identify cell lines with increased sensitivity to AMG-458, a novel selective c-Met inhibitor with radiosensitizing effects. Int J Radiat Oncol Biol Phys 2012,84:e525-531.
2. Liu L, Siegmund A, Xi N, Kaplan-Lefko P, Rex K, Chen A, et al. Discovery of a potent, selective, and orally bioavailable c-Met inhibitor: 1-(2-hydroxy-2-methylpropyl)-N-(5-(7-methoxyquinolin-4-yloxy)pyridin-2-yl)-5-meth yl-3-oxo-2-phenyl-2,3-dihydro-1H-pyrazole-4-carboxamide (AMG 458). J Med Chem 2008,51:3688-3691.
| Cas No. | 913376-83-7 | SDF | |
| Synonyms | AMG 458; AMG458 | ||
| Chemical Name | 1-(2-hydroxy-2-methylpropyl)-N-[5-(7-methoxyquinolin-4-yl)oxypyridin-2-yl]-5-methyl-3-oxo-2-phenylpyrazole-4-carboxamide | ||
| Canonical SMILES | CC1=C(C(=O)N(N1CC(C)(C)O)C2=CC=CC=C2)C(=O)NC3=NC=C(C=C3)OC4=C5C=CC(=CC5=NC=C4)OC | ||
| Formula | C30H29N5O5 | M.Wt | 539.58 |
| Solubility | Soluble 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 | 1.8533 mL | 9.2665 mL | 18.5329 mL |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7066 mL |
| 10 mM | 0.1853 mL | 0.9266 mL | 1.8533 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
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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: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 9 reference(s) in Google Scholar.)
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