| CAS NO: | 1002304-34-8 |
| 规格: | ≥98% |
| 包装 | 价格(元) |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
| 250mg | 电议 |
| 500mg | 电议 |
| Molecular Weight (MW) | 383.4 |
|---|---|
| Formula | C22H17N5O2 |
| CAS No. | 1002304-34-8 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility (In vitro) | DMSO: 0.25 mg/mL (0.65 mM) |
| Water: <1 mg/mL | |
| Ethanol: <1 mg/mL | |
| Solubility (In vivo) | 1% DMSO+30% polyethylene glycol+1% Tween 80: 30 mg/mL |
| Synonyms | AMG 208; AMG-208; AMG208; 4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]-7-methoxyquinoline InChi Key: HEAIZQNMNCHNFD-UHFFFAOYSA-N InChi Code: InChI=1S/C22H17N5O2/c1-28-16-7-8-17-19(13-16)23-12-11-20(17)29-14-22-25-24-21-10-9-18(26-27(21)22)15-5-3-2-4-6-15/h2-13H,14H2,1H3 SMILES Code: COC1=CC=C2C(OCC3=NN=C4C=CC(C5=CC=CC=C5)=NN43)=CC=NC2=C1 |
| In Vitro | In vitro activity: AMG-208 shows the potent inhibition of kinase c-Met activity with IC50 of 9 nM in a cell-free assay. Besides, AMG-208 treatment also leads to the inhibition of HGF-mediated c-Met phosphorylation in PC3 cells with IC50 of 46 nM. Incubation of AMG-208 with rat and human liver microsomes in the presence of NADPH qualitatively yields C6-phenylarene oxidation products as the major metabolites. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation. AMG-208 is identified to be a c-MET and RON dual selective inhibitor. Kinase Assay: AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM. Cell Assay: Pre-incubation of AMG-208 with human liver microsomes for 30 minutes shows a potent time-dependent inhibition for CYP3A4 metabolic activity with IC50 of 4.1 μM, which is an eightfold decrease relative to the IC50 (32 μM) without preincubation. |
|---|---|
| In Vivo | In male Sprague–Dawley rats, AMG-208 (0.5 mg/kg i.v.) shows a high bioavailability with Cl of 0.37 L/h/kg, Vss of 0.38 L/kg and T1/2 of 1 hour, while AMG-208 (2 mg/kg i.v.) shows a bioavailability with AUC0→∞ of 2517 ng·h/mL and F of 43%, respectively. |
| Animal model | Male Sprague-Dawley rats |
| Formulation & Dosage | Dissolved in DMSO; ≤2 mg/kg; i.v. or p.o. |
| References | J Med Chem. 2008 May 22;51(10):2879-82; Bioorg Med Chem Lett. 2009 Nov 15;19(22):6307-12. |
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