Name: CEP-7055
Rating: 5 (10 reviews)

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HIT ID:HIT218963819
Cas No:402857-58-3
常用名:CEP-7055
IUPAC:3-{14-oxo-7-[(propan-2-yloxy)methyl]-3,13-diazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaen-3-yl}propyl 2-(dimethylamino)acetate
IUPAC:3-{14-oxo-7-[(propan-2-yloxy)methyl]-3,13-diazahexacyclo[14.7.0.0^{2,10}.0^{4,9}.0^{11,15}.0^{17,22}]tricosa-1(16),2(10),4(9),5,7,11(15),17(22),18,20-nonaen-3-yl}propyl 2-(dimethylamino)acetate
InChI key:UHEBDUAFKQHUBV-UHFFFAOYSA-N

分子式:C32H35N3O4
分子量:525.649
氢键供体数 (HBD):
氢键受体数 (HBA):
LogP:
SMILES:CC(C)OCc1ccc2n(CCCOC(=O)CN(C)C)c3c4Cc5ccccc5-c4c4C(=O)NCc4c3c2c1
SMILES:CC(C)OCc1ccc2n(CCCOC(=O)CN(C)C)c3c4Cc5ccccc5-c4c4C(=O)NCc4c3c2c1

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.

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