GlpBio

BI-9564

目录号: GC16817纯度: >99.50%
A selective BRD9/7 bromodomain inhibitor
BI-9564
Cas No.: 1883429-22-8
规格价格库存数量操作
5mg¥494.00现货
1
25mg¥2,006.00现货
1
100mg¥5,124.00现货
1
电话: 400-920-5774Email: sales@glpbio.cn

文献被引

本产品暂无引用记录;以下为 GlpBio 产品在 Nature / Cell / Science 等顶刊的客户引用样例
  • Nature cover
    Nature
    641, 529–536 (2025)
  • Nature cover
    Nature
    628, 630–638 (2024)
  • Nature cover
    Nature
    632, 686–694 (2024)
  • Nature cover
    Nature
    618, 1017–1023 (2023)
  • Nature cover
    Nature
    610, 366–372 (2022)
  • Cell cover
    Cell
    187(9):2288-2304 (2024)
  • Cell cover
    Cell
    183(7):1867-1883 (2020)
  • Science cover
    Science
    388(6745) (2025)
  • Science cover
    Science
    387(6739) (2025)
  • Science cover
    Science
    387(6734) (2025)
  • Cell Research cover
    Cell Research
    35, 97–116 (2025)
  • Cell Research cover
    Cell Research
    34, 683–706 (2024)
  • Cell Research cover
    Cell Research
    33, 273–287 (2023)
  • Cell Research cover
    Cell Research
    33, 546–561 (2023)
  • Cell Research cover
    Cell Research
    33, 904–922 (2023)
  • Cell Research cover
    Cell Research
    31, 1291–1307 (2021)

产品描述 Description

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.

实验参考方法 Experimental Reference Method

Cell experiment:

Cells are grown in 50 µL medium as specified by the supplier for 7 days starting with 500 and with 1000 cells per well of a 384 well plate in the presence of varying concentrations of compound before measuring viability via cellular ATP levels using the cell titer glow assay.

Animal experiment:

Female CIEA-NOG mice are engrafted intravenously with 1×107 EOL-1 AML cells stably expressing luciferase and GFP. Following injection of the cells animals are randomized based on body weight (n=10/group). Treatment starts on day 5 with either 0.5% Natrosol or BI-9564 formulated with 0.5% Natrosol. All doses are calculated relative to the mouse body weight on the treatment day. BI-9564 and the vehicle control are administered orally with a dosing volume of 10 mL/kg body weight. BI-9564 is administered daily from day 5 until 17 and from day 20 until 22. Dosing is interrupted on day 18 for two days as one mouse in the treatment group reaches -15% body weight loss. Tumour load is measured 2-3 times weekly based on bioluminescence imaging. The following scoring system is used: score 0, no clinical signs; score 1, tail or hind limb weakness. Animals are sacrificed based on severity criteria including appearance of paralysis score 1 and/or body weight loss exceeding -18%. In S54 this tumor mouse model body weight changes can occur due to increased tumor load or due to intolerability.

References:

[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.
[2]. Rezaul M. Karim, et al. An Advanced Tool To Interrogate BRD9. J. Med. Chem., 2016, 59 (10), pp 4459-4461

产品文档 Product Documents

Purity:>99.50%

化学性质Chemical Properties

CAS 号
1883429-22-8
化学名
4-(4-((dimethylamino)methyl)-2,5-dimethoxyphenyl)-2-methyl-2,7-naphthyridin-1(2H)-one
SMILES
O=C1N(C)C=C(C2=CC(OC)=C(CN(C)C)C=C2OC)C3=CC=NC=C13
分子式
C20H23N3O3
分子量
353.41 g/mol
溶解性
DMF: 5 mg/ml,DMF:PBS(pH 7.2)(1:1): 0.5 mg/ml,DMSO: 5 mg/ml,Ethanol: 2 mg/ml
保存条件
Store at -20°C
General tips
请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。
为了提高溶解度，请将管子加热至 37°C，然后在超声波浴中震荡一段时间。
Shipping Condition
评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备 RT，或根据请求配备蓝冰。

计算工具摩尔浓度 / 稀释 / 分子量 / 单位换算 / 体内配方 / 溶解度

g/mol