溶解性 | DMSO 100 mM Ethanol 100 mM |
存贮条件 | 储存温度2-8℃ |
生化机理 |
I-BET151 is a BET bromodomain inhibitor; I-BET151 blocks recruitment of BET to chromatin. I-BET151 induces apoptosis and G0/G1 cell cycle arrest in MLL-fusion leukemic cell lines in vitro (IC50 values are 15, 26, 120 and 192 nM for NOMO1, MV4;11, MOLM13 and RS4;11 cell lines respectively). I-BET151 reduces BCL2 expression in NOMO1 cells. I-BET151 improves survival in two rodents models of MLL-fusion leukemia in vivo. |
别名 | ;7-(3,5-Dimethyl-4-isoxazolyl)-8-(methyloxy)-1-[(1R)-1-(2-pyridinyl)ethyl]-1,3-dihydro-2H-imidazo[4,5-c]quinolin-2-one,I-BET151 |