Targefrin is a potent EphA2-targeting agent, acts as an antagonist. Targefrin binds EphA2-LBD with 21 nM dissociation constant and an IC50 value of 10.8 nM. Targefrin induces cellular receptor internalization and degradation in several pancreatic cancer cell lines.
Targefrin (0.025-10 μM; 20 min) effectively antagonizes EphA2 degradation in BxPC3 pancreatic cancer cells[1].Targefrin (2-10 μM; 24 h) significantly inhibits pancreatic cancer cell BxPC3 migration[1].
Targefrin (50 mg/kg; i.v.; for 5 days) suppresses tumor growth when conjugated with Paclitaxel[1].
References:
[1]. Baggio C, Udompholkul P, Gambini L, Pellecchia M. Targefrin: A Potent Agent Targeting the Ligand Binding Domain of EphA2. J Med Chem. 2022 Nov 4.