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AMG-208

In stock
Catalog No.
A1186
C-Met inhibitor,potent and highly selective
Grouped product items
SizePriceStock Qty
10mM (in 1mL DMSO)
$120.00
In stock
5mg
$100.00
In stock
25mg
$300.00
In stock
100mg
$800.00
In stock

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Email: [email protected]

Worldwide Distributors

AMG-208 is a highly selective c-Met inhibitor with IC50 value of 9.3 nM [1]. c-Met, the receptor tyrosine kinase, and its natural ligand, hepatocyte growth factor (HGFa), are essential for normal embryonic development and are involved in cell proliferation, migration, and invasion [2].
AMG-208 is a selective c-Met inhibitor. Pre-incubation of AMG-208 with human liver microsomes for 30 minutes inhibited CYP3A4 metabolic activity for eightfold with IC50 value of 4.1 μM in a time-dependent way [1]. In PC3 cells, AMG-208 inhibited HGF-mediated c-Met phosphorylation with IC50 value of 46 nM [2].
In male Sprague-Dawley rats, AMG-208 (0.5 mg/kg i.v.) displays a high bioavailability with Cl value of 0.37 L/h/kg, Vss value of 0.38 L/kg and T1/2 value of 1 hour [2]. Deregulation of c-Met has been involved in several human cancers and AMG-208 can inhibit c-Met activity, which would be used for cancer treatment [2].
References:
[1]. Boezio AA, Berry L, Albrecht BK, et al. Discovery and optimization of potent and selective triazolopyridazine series of c-Met inhibitors. Bioorg Med Chem Let,. 2009, 19(22): 6307-6312.
[2]. Albrecht BK, Harmange JC, Bauer D, 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.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt383.4
Cas No.1002304-34-8
FormulaC22H17N5O2
Solubility≥3.83mg/mL in DMSO
Chemical Name7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
SDFDownload SDF
Canonical SMILESCOC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5
Shipping ConditionEvaluation sample solution : ship with blue ice.All other available size: ship with RT , or blue ice upon request
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.

Biological Activity

Description AMG-208 is a potent and highly selective inhibitor of Met with IC50 value of 9.3 nM.
Targets Met          
IC50 9.3 nM          

Quality Control

Quality Control & MSDS

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Chemical structure

AMG-208