Gilteritinib is a small-molecule FLT3/AXL inhibitor with IC50 values of 0.29 nM and 0.73 nM for FLT3 and AXL, respectively. It inhibits FLT3 at an IC50 value that was approximately 800-fold more potent than the concentration required to inhibit c-KIT (230 nM).
SGI-7079, a novel selective Axl inhibitor with an IC50 of 58 nM in vitro, inhibits tumor growth in a dose dependent manner and is a potential therapeutic target for overcoming EGFR inhibitor resistance.
PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
AG-18 inhibits EGFR with IC50 of 35 μM.
Butein, a plant polyphenol isolated from Rhus verniciflua, is able to inhibit the activation of protein tyrosine kinase, NF-κB and STAT3, also inhibits EGFR.
ASP3026 is a novel and selective inhibitor for ALK with IC50 of 3.5 nM.
AMG 337 is an oral, small molecule, ATP-competitive, highly selective inhibitor of the MET receptor with an IC50 of 1 nM.
BAW2881 is a novel vascular endothelial growth factor (VEGF) receptor tyrosine-kinase inhibitor that potently inhibits VEGFR1-3 at 1.0-4.3 nanomolar (nM) concentrations and inhibits PDGFRβ, c-Kit, and RET at 45-72 nM concentrations.