MET kinase-IN-4 is an orally active Met kinase inhibitor. MET kinase-IN-4 has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM. MET kinase-IN-4 can be used for the research of cancer.
MET kinase-IN-4 (Compound 2) has potent Met kinase inhibitory activity with an IC50 value of 1.9 nM[1].MET kinase-IN-4 inhibits Flt-3 and VEGFR-2 kinases with IC50 values of 4 and 27 nM, respectively[1]. MET kinase-IN-4 (3 μM) shows good metabolic stability in both human and mouse liver microsomes[1].
MET kinase-IN-4 (Compound 2) (i.v., p.o.; 5, 10 mg/kg) possesses a favorable pharmacokinetic profile in mice[1].MET kinase-IN-4 (p.o.; 6.25, 12.5, 25 and 50 mg/kg; once a day) demonstrates significant in vivo antitumor activity in the GTL-16 human gastric carcinoma xenograft model[1].
References:
[1]. Kyoung Soon Kim, et al. Discovery of pyrrolopyridine-pyridone based inhibitors of Met kinase: synthesis, X-ray crystallographic analysis, and biological activities. J Med Chem. 2008 Sep 11;51(17):5330-41.