1002304-34-8

1002304-34-8 structure

Name: AMG-208
Chemical Name: 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
CAS Number: 1002304-34-8
Molecular Formula: C₂₂H₁₇N₅O₂
Molecular Weight: 383.403
Catalog: Biochemical Inhibitor Protein tyrosine kinase
Create Date: 2018-05-17 08:00:00
Modify Date: 2024-01-10 17:32:08
AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.IC50 value: 9.3 nMTarget: c-Metin 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].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].

Name	7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
Synonyms	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 AMG208,AMG-208 S1316_Selleck Quinoline, 7-methoxy-4-[(6-phenyl-1,2,4-triazolo[4,3-b]pyridazin-3-yl)methoxy]- 3cd8 Triazolopyridazine,4 AMG-208 AMG208

Description	AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.IC50 value: 9.3 nMTarget: c-Metin 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].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].
Related Catalog	Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR Research Areas >> Cancer
References	[1]. Albrecht BK, et al. Discovery and optimization of triazolopyridazines as potent and selective inhibitors of the c-Met kinase. J Med Chem. 2008, 51(10), 2879-2882. [2]. Boezio AA, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Lett. 2009, 19(22), 6307-6312. [3]. Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45.

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