LDN-211904 oxalate (compound 32) is a potent and selective EphB3 inhibitor with an IC50 of 0.079 μM. LDN-211904 oxalate shows good metabolic stability in mouse liver microsomes. LDN-211904 oxalate with cetuximab could be effective in inhibiting STAT3-activated CSC stemness and cetuximab resistance in CRC.