NCIt definition : An orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like
activity of the proteasome, with potential antineoplastic activity. Delanzomib represses
the proteasomal degradation of a variety of proteins, including inhibitory kappaBalpha
(IkappaBalpha), resulting in the cytoplasmic sequestration of the transcription factor
NF-kappaB; inhibition of NF-kappaB nuclear translocation and transcriptional up-regulation
of a variety of cell growth-promoting factors; and apoptotic cell death in susceptible
tumor cell populations. In vitro studies indicate that this agent exhibits a favorable
cytotoxicity profile toward normal human epithelial cells, bone marrow progenitors,
and bone marrow-derived stromal cells relative to the proteasome inhibitor bortezomib.
The intracellular protein IkappaBalpha functions as a primary inhibitor of the proinflammatory
transcription factor NF-kappaB.;
UNII : 6IF28942WO;
InChIKey : SJFBTAPEPRWNKH-CCKFTAQKSA-N;
CAS number : 847499-27-8;
Molecule name : CEP 18770; CEP-18770; CT-47098; NPH-007098;