AP1903 (Rimiducid, AP-1903) is a potent, specific synthetic ligand of FKBP Phe36Val mutant (F36V-FKBP) with binding IC50 of 1.8 nM; displaces the Fluoresceinated FK506 probe from F36V-FKBP with an IC50 of 5 nM, but shows negligible binding activity to the wild-type protein; elicited potent and dose-dependent apoptotic death of human fibrosarcoma line HT1080 expressing dimerizer-dependent Fas constructs with EC50 of 0.1 nM; induces activation of Fas signaling both in vitro and in vivo, AP1903 is a lipid-permeant dimerizing ligand induced oligomerization and activation of FKBP.
Blood Cancer
Phase 3 Clinical
