BI-9564

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Chemical Structure| 1883429-22-8 同义名 : -
CAS号 : 1883429-22-8
货号 : A429986
分子式 : C20H23N3O3
纯度 : 98%
分子量 : 353.41
MDL号 : MFCD30182324
存储条件：

Pure form Sealed in dry, 2-8°C

In solvent -20°C:3-6个月-80°C:12个月
溶解度 : -
动物实验配方：
生物活性
靶点

  • BET

    BRD7, Kd:73 nM

    BRD9, Kd:5.9 nM

  • bromodomain

    CECR2, Kd:77 nM
描述 Recurrent mutations in the subunits of the mammalian switch/sucrose nonfermentable complex have been observed in different types of tumors. Bromodomains are protein-binding domains with an affinity to lysine-acetylated target proteins. BI-9564 is a potent, selective inhibitor of BRD9 and BRD7 bromodomains with IC50 values of 75nM and 3.41μM, respectively. The IC50 values of BI-9564 for BRD4-BD1, BRD4-BD2, and BRD2-BD1 were above 100μM. BI-9564 binds to BRD9 and BRD7 with KD values of 14nM and 239nM, respectively. In U2OS cells, BI-9564 inhibited BRD9 at a concentration of 100nM. No toxicity was observed in U2OS cells after 24-h exposure of BI-9564. BI-9564 inhibited proliferation of human acute myeloid eosinophilic leukemia cell line EOL-1 with an EC50 value of 800nM. In a xenograft model of human acute myeloid leukemia, daily oral treatment with BI-9564 (180mg/kg) for 12 days significantly reduced tumor growth with a tumor growth inhibition value of 52% as compared to the vehicle-treated group[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.83mL

0.57mL

0.28mL

14.15mL

2.83mL

1.41mL

28.30mL

5.66mL

2.83mL
参考文献

[1]Laetitia J M, Manfred K, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016 May 26; 59(10): 4462–4475.

[2]Karim RM, Schonbrunn E. An Advanced Tool To Interrogate BRD9. J Med Chem. 2016 May 26;59(10):4459-61.

[3]Martin LJ, Koegl M, Bader G, et al. Structure-Based Design of an in Vivo Active Selective BRD9 Inhibitor. J Med Chem. 2016;59(10):4462-4475. doi:10.1021/acs.jmedchem.5b01865