1174046-72-0

Biologieal

GSK1363089 (XL880)is an orally bioavailable，small molecule MET/VEGFR2 inhibitor with potential antineoplastic activity. This compound binds to and selectively inhibits HGF receptor c-MET(IC50 of 0.4 nM)and VEGFR2, which may result in the inhibition of tumor angiogenesis, tumor cell proliferation and metastasis. ^[1]
A Multicenter Phase II Study shows that plasma levels of GSK1363089 reach ~250 ng/mL at Day 5 but drop to baseline levels by the start of the next cycle. ED50 done for gastric cancer xenograft inhibition is ≥ 0.3 μM (~150 ng/mL). ^[1]

Reference

ASCO Annual Meeting. Citation:J Clin Oncol 26: 2008 (May 20 suppl; abstr 5103)