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BI-9564
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BI-9564图片
CAS NO:1883429-22-8
规格:98%
分子量:353.41
包装与价格:
包装价格(元)
5mg电议
25mg电议
100mg电议

产品介绍
BRD9/7 specific inhibitor
CAS:1883429-22-8
分子式:C20H23N3O3
分子量:353.41
纯度:98%
存储:Store at -20°C

Background:

IC50: 75 nM and 3.4 μM for BRD9 and BRD7 bromodomains, respectively


BI-9564 is a BRD9/7 specific inhibitor.


BRD7 and BRD9 are two important members of the bromodomain family protein. Both BRD7 and BRD9 have been implicated in chromatin remodeling.


In vitro: BI-9564 was identified as a BRD9/7 specific inhibitor via fragment-based screening and structure-guided design. BI-9564 was found to be bind to BRD9 with a higher affinity than to BRD7, and was negative on BET family proteins. In addition, BI-9564 demonstrated in vitro off-target selectivity to CECR2, but not in cells [1].


In vivo: In animal study, BomTac:NMRIFoxn1nu mice were given two oral doses daily and the concentration of BI-9564 in plasma was measured. Dose-dependent AUCs were obtained for BI-9564, achieving exposures that were higher compared to the EC50 level for EOL-1 cells. Moreover, when the oral treatment with BI-9564 at 180 mg/kg was initiated on day 5 and applied daily with an interruption at day 18 and 19, a significant reduction in tumour growth compared to controls was found on day 18 leading to a median tumour growth inhibition value of 52% [1].


Clinical trial: Up to now, BI-9564 is still in the preclinical development stage.


Reference:
[1] Martin LJ et al.  Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26;59(10):4462-75.