I-BET151

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

I-BET151 (GSK1210151A) 是一种有效的选择性 BET 溴结构域抑制剂。

I-BET151 (GSK1210151A) is a potent, selective BET bromodomain inhibitor with IC50 of 0.5, 0.25 and 0.79 uM for BRD2, BRD3 and BRD4 in FP assays, shows no effect on the 23 other bromodomain proteins including MLL; demonstrates potent efficacy against cell lines harbouring different MLL-fusions (MOLM13 cell IC50=120 nM, MV4:11 cell IC50=26 nM), induices early cell cycle arrest and apoptosis, selectively abrogates BRD3/4 recruitment to chromatin;shows significant therapeutic value and survival benefit in mouse models of murine MLL-AF9 and human MLL-AF4 leukaemia.

Cell Viability Assay Cell Line:H929 cells Concentration:1 μM Incubation Time:72 hours Result:Displays the majority of live cells resided in the G0 phase and commensurate with a dose- and time-dependent decrease in cell proliferation and abrogation of bromodeoxyuridine incorporation.Cell Proliferation Assay Cell Line:H929 cells Concentration:100 nM Incubation Time:72 hours Result:Caused a significant dose- and time-dependent decrease in the proportion of myeloma cells in S/G2 phase.

Animal Model:Mice (model of subcutaneous myeloma)Dosage:50 mg/kg Administration:I.p.; daily for 21 daysResult:Reduced rate of tumor size doubling than vehicle-treated mice.

GSK1210151A | I-BET 151 | GSK-1210151A

Chromatin/Epigenetic

Bromodomain

BRD2|BRD3|BRD4

Cancer

——

1300031-49-5

415.4445

C23H21N5O3

>98% (HPLC)

10 mM in DMSO

O=C(N1[C@@H](C2=NC=CC=C2)C)NC3=C1C4=CC(OC)=C(C5=C(C)ON=C5C)C=C4N=C3

2H-Imidazo[4,5-c]quinolin-2-one, 7-(3,5-dimethyl-4-isoxazolyl)-1,3-dihydro-8-methoxy-1-[(1R)-1-(2-pyridinyl)ethyl]-

(-20℃)

With Ice Pack

≥ 2 years