产品描述:
Flavopiridol is an orally bioavailable inhibitor of cyclin dependent kinases (IC50s = ~100, ~100, ~100, and 300 nM for Cdk1, Cdk2, Cdk4, and Cdk7, respectively).{23163} It also inhibits TEFb, a complex composed of Cdk9 and cyclin T1, with a Ki value of 3 nM.{23157} Flavopiridol inhibits transcription of a CMV promoter in HeLa nuclear extract (IC50 = 34 nM), Tat-stimulated transcription of an HIV-1 promotor (IC50 = 7 nM), and HIV-1 replication in HEK293T cells (IC50 = In vivo, flavopiridol (5 mg/kg, i.p.) induces apoptosis and cyclin D1 depletion and delays tumor growth in an HN-12 head and neck carcinoma mouse xenograft model.{23163} It also suppresses synovial hyperplasia and joint destruction in a mouse model of collagen-induced arthritis.{23156}