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| Cas No.: | 1002304-34-8 |
| Chemical Name: | 7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline |
| Synonyms: | AMG208; AMG 208 |
| SMILES: | COC1=CC=C2C(OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5)=CC=NC2=C1 |
| Formula: | C22H17N5O2 |
| M.Wt: | 383.4 |
| Sotrage: | 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO |
| Description: | AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM. |
| 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[1]. |
| In Vitro: | 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 [1]. 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 [2]. AMG-208 is identified to be a c-MET and RON dual selective inhibitor [3]. |