AMG-208

Product NameAMG-208
CAS1002304-34-8
MFC22H17N5O2
MW383.4
EINECS
MOL File1002304-34-8.mol

Chemical Properties

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

Usage And Synthesis

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