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AMG-208

Catalog No.GC12600

AMG-208 est un inhibiteur sélectif double c-Met/RON actif par voie orale avec une IC50 de 9 nM pour c-Met. L'AMG-208 est un inhibiteur du CYP3A4 avec une IC50 de 32 μM. AMG-208 a une activité anticancéreuse.

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AMG-208 Chemical Structure

Cas No.: 1002304-34-8

Taille Prix Stock Qté
10mM (in 1mL DMSO)
89,00 $US
En stock

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Sample solution is provided at 25 µL, 10mM.

Product Documents

Quality Control & SDS

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Background

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

Cas No. 1002304-34-8 SDF
Chemical Name 7-methoxy-4-[(6-phenyl-[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy]quinoline
Canonical SMILES COC1=CC2=NC=CC(=C2C=C1)OCC3=NN=C4N3N=C(C=C4)C5=CC=CC=C5
Formula C22H17N5O2 M.Wt 383.4
Solubility ≥ 3.83mg/mL in DMSO Storage Store at -20°C
General tips Please select the appropriate solvent to prepare the stock solution according to the solubility of the product in different solvents; once the solution is prepared, please store it in separate packages to avoid product failure caused by repeated freezing and thawing.Storage method and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored at -20°C, please use it within 1 month.
To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time.
Shipping Condition Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request.

Complete Stock Solution Preparation Table

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1 mg 5 mg 10 mg
1 mM 2.6082 mL 13.0412 mL 26.0824 mL
5 mM 0.5216 mL 2.6082 mL 5.2165 mL
10 mM 0.2608 mL 1.3041 mL 2.6082 mL
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Average Rating: 5 ★★★★★ (Based on Reviews and 26 reference(s) in Google Scholar.)

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