||Altiratinib(DCC-2701) is a novel c-MET/TIE-2/VEGFR inhibitor; effectively reduce tumor burden in vivo and block c-MET pTyr(1349)-mediated signaling, cell growth and migration as compared with an HGF antagonist in vitro.
||Foretinib is an ATP-competitive inhibitor of HGFR and VEGFR, with IC50 of 0.4 nM and 0.9 nM. Foretinib is an orally bioavailable small molecule with potential antineoplastic activity.
||GSK1070916 is a reversible and ATP-competitive inhibitor of Aurora B/C with IC50 of 3.5 nM/6.5 nM. It displays >100-fold selectivity against the closely related Aurora A-TPX2 complex. Phase 1.
||Tie2 kinase inhibitor
||Tie2 kinase inhibitor， an optimized compound of SB-203580, is selective to Tie2 with IC50 of 0.25 μM, which is 200-fold more effective than p38.
||NVP-BHG712 is a specific EphB4 inhibitor with ED50 of 25 nM that discriminates between VEGFR and EphB4 inhibition; also shows activity against c-Raf, c-Src and c-Abl with IC50 of 0.395 μM, 1.266 μM and 1.667 μM, respectively.
||ACTB-1003 is an oral kinase inhibitor (IC50: 6/2/4 nM, for FGFR1/VEGFR2/Tie-2).