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AMG-208

Names

[ CAS No. ]:
1002304-34-8

[ Name ]:
AMG-208

[Synonym ]:
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

Biological Activity

[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.


[Related Small Molecules]

Capmatinib (INCB28060) | Foretinib (GSK1363089) | PHA-665752 | BMS-777607 | Dihexa | Savolitinib | Tivantinib (ARQ 197) | tepotinib | LY2801653 | SGX-523 | DCC-2618 | SU11274 | Ensartinib | CEP-40783 | JNJ-38877605

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Molecular Formula ]:
C22H17N5O2

[ Molecular Weight ]:
383.403

[ Exact Mass ]:
383.138214

[ PSA ]:
74.43000

[ LogP ]:
4.02

[ Index of Refraction ]:
1.696

[ Storage condition ]:
-20℃

Safety Information

[ Hazard Codes ]:
N

Related Compounds