LY-2510924 (LY2510924) is a potent and selective, cyclic peptide CXCR4 antagonist with IC50 of 0.079 nM, without apparent agonist activity.
LY-2510924 inhibits SDF-1-induced cell migration with IC50 of 0.26 nM and inhibits SDF-1/CXCR4-mediated intracellular signaling.
LY-2510924 exhibits inhibition of SDF-1-stimulated phospho-ERK and phospho-Akt in tumor cells.
LY-2510924 shows inhibition of tumor growth in human xenograft models with acceptable in vivo stability and a pharmacokinetic profile.
