CPI203

别名

(6S)-4-(4-Chlorophenyl)-2,3,9-trimethyl-6H-thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide

生化/生理作用

CPI203 is an analog of the BET inhibitor (BETi) (+)-JQ1 and is bioavailable via oral or intraperitoneal administration. It plays an important role in lenalidomide and dexamethasone functions in in vitro and in vivo models of multiple myeloma. CPI203 inhibits proliferation, apoptosis and cell cycle arrest in A431 cell line and primary skin squamous cell carcinoma (SCC) cells. CPI203 is an inhibitor of BRD4, a bromodomain-containing protein that binds to histones to regulate recruitment of transcription factors. BRD4 is also an RNA Pol II kinase. CPI203 blocks BRD4 kinase activity in cells and in vivo. It has shown synergistic antitumor activity with lenalidomide in bortezomib-resistant mantle cell lymphoma.