| Identification | Back Directory | [Name]
AMG-208 | [CAS]
1002304-34-8 | [Synonyms]
CS-191
AMG-208
AMG-208, >=98%
AMG208; AMG 208
AMG-208 USP/EP/BP
AMG-208;AMG208; AMG 208
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 | [Molecular Formula]
C22H17N5O2 | [MDL Number]
MFCD17215205 | [MOL File]
1002304-34-8.mol | [Molecular Weight]
383.41 |
| Chemical Properties | Back Directory | [density ]
1.34 | [storage temp. ]
Store at -20°C | [solubility ]
insoluble in EtOH; insoluble in H2O; ≥3.83 mg/mL in DMSO | [form ]
solid | [pka]
5.98±0.27(Predicted) | [color ]
White to off-white |
| Hazard Information | Back Directory | [Uses]
AMG-208 is an orally active c-Met/RON dual selective inhibitor with an IC50 of 9 nM for c-Met. AMG-208 is a CYP3A4 inhibitor with an IC50 of 32 μM. AMG-208 has anti-cancer activity[1][2][3]. | [Definition]
ChEBI: A member of the class of quinolines that is 7-methoxyquinoline substituted at position 4 by a (6-phenyl[1,2,4]triazolo[4,3-b]pyridazin-3-yl)methoxy group. AMG exhibits antitumour activity, particularly in prostate cancer. | [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].
| [target]
Met | [IC 50]
CYP3A4: 32 μM (IC50); c-Met: 9 nM (IC50) | [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. DOI:10.1021/jm800043g
[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. DOI:10.1016/j.bmcl.2009.09.096
[3] Liu X, et al. Developing c-MET pathway inhibitors for cancer therapy: progress and challenges. Trends Mol Med. 2010,16(1), 37-45. DOI:10.1016/j.molmed.2009.11.005 |
|
|