The GI50 is calculated as the concentration that produced 50 % growth inhibition. Values are represented using untreated control cells. MTT is added for 2-6 additional hours before spectrophotometric measurement. MCL primary cells and cell lines are incubated as indicated with lenalidomide and/or CPI203.
Calcusyn software version 2.0 serial#
IC50 values are calculated using a 10-point serial dilution of BET inhibitor.Ģ PBMC cultures from healthy donors and 9 MCL cell lines (Granta-519, JVM-2, UPN1, Z-138, JeKo-1, ZBR, JBR, Mino, REC-1 cells) The BRD4 α-screen assay is a proximity-based assay using a tetraacteylated H4 peptide and the isolated bromodomain 1 of human BRD4. In REC-1 tumor-bearing mice, the combination of lenalidomide with CPI203 (2.5 mg/kg i.p.) synergistically augments the antitumoral properties of each single agent via the abrogation of MYC and IRF4 expression and the induction of apoptosis. īRD4 mediates CTD Ser2 phosphorylation in vivo. Furthermore, lenalidomide and CPI203, by targeting IRF4 and MYC, efficiently activates the cell death program in MCL cells resistant to bortezomib. CPI203 exerts a cytostatic effect in all the 9 MCL cell lines analyzed with GI50 ranging from 0.06 to 0.71 μM, with low cytotoxicity in normal PBMCs from healthy donors. CPI-203 is a potent BET bromodomain inhibitor with IC50 of 37 nM for BRD4.ĬPI203 inhibits BRD4 in vitro and in cells, while does not affect BRD4 kinase activity in vitro.
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