Delanzomib (CEP18770) is a potent, orally active proteasome inhibitor with IC50 of 3.8 nM against chymotrypsin-like proteasome activity.
Delanzomib demonstrates marginal inhibition of the tryptic and peptidyl glutamyl activities of the proteosome.
Delanzomib down-modulates the NF-kappaB activity and the expression of several NF-kappaB downstream effectors, induces apoptotic cell death in MM cells.
Delanzomib demonstrates tumor regression in MM xenografts with favorable tumor selectivity profile.
