N-[4-[(2-Amino-3-chloropyridin-4-yl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-1,2-dihydropyridine-3-carboxamide

Uses

N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-1,2-dihydro-2-oxo-3-pyridinecarboxamide is a selective and orally efficacious Inhibitor of the Met Kinase superfami ly.

Definition

ChEBI: N-[4-[(2-amino-3-chloro-4-pyridinyl)oxy]-3-fluorophenyl]-4-ethoxy-1-(4-fluorophenyl)-2-oxo-3-pyridinecarboxamide is an aromatic amide.

Biological Activity

bms 777607 is a novel, selective and orally available atp-competitive met kinase inhibitor that primarily targets several met family members, including ron, met, tyro-3 and axi, with half maximal inhibitory concentration ic50 of 1.8 nmol/l, 3.9 nmol/l, 4.3 nmol/l and 1.1 nmol/l respectively. moreover, at higher concentrations, bms 777607 has been found to inhibit other protein tyrosine kinases, including mer, flt-3, aurora b, lck and vegfr2 with ic50 of 14 nmol/l, 16 nmol/l, 78 nmol/l, 120 nmol/l and 180 nmol/l respectively. in previous studies, bms 777607 potently inhibited the auto-phosphorylation of c-met (ic50: 20 nmol/l) leading to impaired xenograft growth.small-molecule inhibitor bms-777607 induces breast cancer cell polyploidy with increased resistance to cytotoxic chemotherapy agents. mol cancer ther. 2013 may;12(5):725-36. doi: 10.1158/1535-7163.mct-12-1079. epub 2013 mar 6.

References

[1]dai y, siemann dw. bms-777607, a small-molecule met kinase inhibitor, suppresses hepatocyte growth factor-stimulated prostate cancer metastatic phenotype in vitro. mol cancer ther. 2010 jun;9(6):1554-61. doi: 10.1158/1535-7163.mct-10-0359. epub 2010 jun 1.
[2]sharma s, zeng jy, zhuang cm, zhou yq, yao hp, hu x, zhang r, wang mh.