1002304-34-8
7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline
CAS: 1002304-34-8
Molecular Formula: C22H17N5O2
1002304-34-8 - Names and Identifiers
1002304-34-8 - Physico-chemical Properties
| Molecular Formula | C22H17N5O2 |
| Molar Mass | 383.4 |
| Density | 1.34 |
| pKa | 5.98±0.27(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | AMG-208 effective inhibition of kinase c-Met activity, IC50 9 nM. In addition, AMG-208 action on PC3 cells also inhibited HGF-regulated phosphorylation by c-Met with an IC50 of 46 nM. In the presence of NADPH, AMG-208 was incubated with rat and human liver microparticles, resulting in C6-phenylarene oxidation. AMG-208 pre-incubation with human liver microsomes for 30 minutes inhibits CYP3A4 metabolic activity in a time-dependent manner with an IC50 of 4.1 μm, which is about 8-fold lower than that without pre-incubation, the IC50 in the absence of pre-incubation was 32 μm. AMG-208 as a c-MET and RON dual selective inhibitor. AMG-208 effectively inhibited kinase c-Met activity with IC50 of 9 nM. In addition, AMG-208 action on PC3 cells also inhibited HGF-regulated phosphorylation by c-Met with an IC50 of 46 nM. In the presence of NADPH, AMG-208 was incubated with rat and human liver microparticles, resulting in C6-phenylarene oxidation. AMG-208 pre-incubation with human liver microsomes for 30 minutes inhibits CYP3A4 metabolic activity in a time-dependent manner with an IC50 of 4.1 μm, which is about 8-fold lower than that without pre-incubation, the IC50 in the absence of pre-incubation was 32 μm. AMG-208 as a c-MET and RON dual selective inhibitor. |
| In vivo study | AMG-208, the male Sprague-Dawley rats were injected with 0.5 mg/kg japonica rice porridge, which had significant bioavailability, Cl was 0.37 L/h/kg, Vss was 0.38 L/kg, t1/2 was 1 hour, however AMG-208, treated intravenously at a dose of 2 mg/kg, also had bioavailability, AUC0 → ∞ was 2517 ng · hour/mL,F was 43%. AMG-208, a dose of 0.5 mg/kg of Japonica rice porridge was administered to male Sprague Dawley rats with significant bioavailability, Cl 0.37 L/h/kg, V ss is 0.38 L/kg , T 1/2 is 1 hour, however AMG-208 intravenous treatment at a dose of 2 mg/kg, also has biological effectiveness, AUC 0 → ∞ was 2517 ng · hour/mL,F was 43%. |
1002304-34-8 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.608 ml | 13.041 ml | 26.082 ml |
| 5 mM | 0.522 ml | 2.608 ml | 5.216 ml |
| 10 mM | 0.261 ml | 1.304 ml | 2.608 ml |
| 5 mM | 0.052 ml | 0.261 ml | 0.522 ml |
Last Update：2024-01-02 23:10:35
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View History
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