| Description |
T-1840383 is a potent, ATP-competitive, dual c-Met/VEGFR-2 inhibitor with IC50 of 1.9, 7.7, 2.2 and 5.5 nM for c-Met, VEGFR1, 2 and 3, respectively; also potently inhibit several kinases including c-Mer, Ret, Ron, Rse, Tie-2, and TrkA as well as mutants of Abl, c-Kit, FGFR2, and PDGFRα with IC50 of <10 nM; inhibits HGF-stimulated c-Met phosphorylation (IC50=8.8 nM) in A549 cells, inhibits c-Met–dependent cell proliferation in vitro, inhibits VEGF receptor-2 phosphorylation and VEGF signaling in HUVECs; shows potent antitumor efficacy in a wide variety of human tumor xenograft mouse models, along with reduction of c-Met phosphorylation levels and microvessel density within tumor xenografts.
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