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BI-7273
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-7273图片
CAS NO:1883429-21-7
规格:98%
分子量:353.41
包装与价格:
包装价格(元)
5mg电议
25mg电议

产品介绍
BRD9 bromodomain inhibitor
CAS:1883429-21-7
分子式:C20H23N3O3
分子量:353.41
纯度:98%
存储:Store at -20°C

Background:

IC50: 19 and 117 nM for BRD9 and BRD7, respectively.


BI-7273 is a BRD9 bromodomain inhibitor.


BRD9, a SWI/SNF subunit, is identified to have a key role in leukemia growth, and the BRD9 bromodomain (BD) has been shown to be critical for the proliferation of acute myeloid leukemia cells.


In vitro: BI-7273 was previously demonstrated to mimic genetic perturbation of BRD9. BI-7273 could also target BRD7 BD, a BD protein that was found in a subclass of SWI/SNF remodelling complexes sharing high sequence homology with BRD9. In addition, BI-7273 was able to form an additional positive interaction with the carbonyl of Asn100 in BRD9. Furthermore, BI-7273 showed no measurable activity against BET family BDs even up to a concentration of 100 μM in the biochemical Alpha assay [1].


In vivo: In order to explore the potential of BI-7273 as in-vivo chemical probe, female BomTac:NMRIFoxn1nu mice was orally administered two doses at 20 and 180 mg/ kg and the concentration of BI-7273 in plasma over time was measured. Results showed that dose-dependent but nonlinear AUC was observed for BI-7273, achieving exposure that was higher compared to the EC50 level determined for BI-7273 in proliferation assays with EOL-1 cells [1].


Clinical trial: Up to now, BI-7273 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.