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CEP-7055

CAT: 0931-T69288-01Size: 25 mgDry Ice: NoHazardous: No
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CAT#:0931-T69288-01Size:25 mg
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24/48H Stock Items & 2 to 6 Weeks non Stock Items.
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CAS Number
402857-58-3
Target
Others, VEGFR
Related Pathways
Tyrosine Kinase/Adaptors, Others, Angiogenesis
Bioactivity
CEP-18770 is an orally bioavailable synthetic P2 threonine boronic acid inhibitor of the chymotrypsin-like activity of the proteasome, with potential antineoplastic activity. Proteasome inhibitor CEP 18770 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.
Smiles
C(CCOC(CN(C)C)=O)N1C=2C(=C3C(=C4C2CC=5C4=CC=CC5)C(=O)NC3)C=6C1=CC=C(COC(C)C)C6
Molecular Formula
C32H35N3O4
Molecular Weight
525.64
Shipping Conditions
Ice Packs
Storage Temperature
-20°C