1002304-34-8

1002304-34-8 - Names and Identifiers

Name	7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline
Synonyms	CS-191 AMG208 AMG 208 AMG-208 AMG 208 7-Methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline 7-methoxy-4-((6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy)quinoline Quinoline, 7-Methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)Methoxy]- 7-Methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline AMG 208
CAS	1002304-34-8

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%.