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BRD4 Inhibitor-10

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Chemical Structure| 1660117-38-3 同义名 : Bi 894999
CAS号 : 1660117-38-3
货号 : A982874
分子式 : C25H27N5O2
纯度 : 97%
分子量 : 429.514
MDL号 : MFCD32067915
存储条件：

粉末 Sealed in dry,Store in freezer, under -20°C

液体 -20°C:3-6个月-80°C:12个月
溶解度 :

DMSO: 120 mg/mL(279.39 mM)，配合低频超声助溶，注意：DMSO长时间开封后，会吸水并导致溶解能力下降，请避免使用长期开封的DMSO
动物实验配方：
生物活性
靶点

  • BET

    BRD4-BD1, IC50:5 nM

    BRD4-BD2, IC50:41 nM
描述 Bromodomain and extra-terminal domain (BET) proteins consist of four mammalian members (BRD2, BRD3, BRD4, and BRDT), which play a pivotal role in the transcriptional regulation of the inflammatory response[1].In contrast to BI 894999, volasertib treatment neither affects MYC nor HEXIM1 expression, but augments and prolongs the decrease of MYC expression caused by BI 894999 treatment. In vitro combination of both compounds leads to a decrease in S-Phase and to increased apoptosis. In vitro scheduling experiments guided in vivo experiments in disseminated AML mouse models. Co-administration of BI 894999 and volasertib dramatically reduces tumor burden accompanied by long-term survival of tumor-bearing mice and eradication of AML cells in mouse bone marrow[2]. In preclinical studies, BI 894999 is highly active in AML cell lines, primary patient samples, and xenografts. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state. BI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors[3].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

2.33mL

0.47mL

0.23mL

11.64mL

2.33mL

1.16mL

23.28mL

4.66mL

2.33mL
参考文献

[1]Lei Liu, Changjun Yang, Eduardo Candelario-Jalil. Role of BET Proteins in Inflammation and CNS Diseases. Front Mol Biosci. 2021 Sep 16;8:748449.Review of poly (ADP-ribose) polymerase (PARP) mechanisms of action and rationale for targeting in cancer and other diseases. Crit Rev Eukaryot Gene Expr. 2014;24(1):15-28.

[2] Ulrike Tontsch-Grunt, Dorothea Rudolph,et al. Synergistic activity of BET inhibitor BI 894999 with PLK inhibitor volasertib in AML in vitro and in vivo. Cancer Lett. 2018 May 1;421:112-120.

[3] Daniel Gerlach, Ulrike Tontsch-Grunt,et al. The novel BET bromodomain inhibitor BI 894999 represses super-enhancer-associated transcription and synergizes with CDK9 inhibition in AML.Oncogene. 2018 May;37(20):2687-2701.