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CAS No.: 1883429-22-8

BI-9564 Catalog No. CSN18952

Synonyms: BI-9564

BI-9564 is an inhibitor of BRD9 (IC50 = 75 nM) and BRD7 (IC50 = 3.4 µM).

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400-920-2911

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实验方案

技术信息

生物活性

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 K_D 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].
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

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.8295 mL
- 14.1477 mL
- 28.2954 mL
- 5 mM
- 0.5659 mL
- 2.8295 mL
- 5.6591 mL
- 10 mM
- 0.2830 mL
- 1.4148 mL
- 2.8295 mL

技术信息

CAS号

1883429-22-8

储存条件

粉末: Sealed in dry,2-8°C

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H23N3O3

运输

蓝冰

分子量

353.41

别名

BI-9564

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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