| 货号 | 规格 | 价格 | 上海 | 北京 | 武汉 | 南京 | 购买数量 |
|---|---|---|---|---|---|---|---|
S89335-5mg |
98.3% | ￥450.00 | 6 | - | - | - |
|
S89335-10mg |
98.3% | ￥720.00 | 6 | - | - | - |
|
S89335-25mg |
98.3% | ￥1440.00 | 6 | - | - | - |
|
S89335-100mg |
≥98% | ￥3690.00 | 货期：2-3天 | - | - | - |
|
BI 894999 是一种有效的、选择性的 BET 抑制剂，可抑制BRD4-BD1和BRD4-BD2与乙酰化组蛋白的结合，对应的IC50值分别为5 nM和41 nM。BI 894999 对BRD2/3/4和BRDT (Kd为0.49-1.6 nM) 具有高度选择性，相对于BRD4-BD1具有至少200倍的选择性
| 产品描述： | BI 894999 是一种有效的、选择性的 BET 抑制剂，可抑制BRD4-BD1和BRD4-BD2与乙酰化组蛋白的结合，对应的IC50值分别为5 nM和41 nM。BI 894999 对BRD2/3/4和BRDT (Kd为0.49-1.6 nM) 具有高度选择性，相对于BRD4-BD1具有至少200倍的选择性 | ||||||||||||||||||||
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| 靶点： | BET; BRD4-BD1(Cell-free assay):5 nM; BRD4-BD2(Cell-free assay):41 nM;EpigeneticReaderDomain | ||||||||||||||||||||
| 体外研究： | BI 894999 is highly active in AML cell lines, primary patient samples. BI 894999 targets super-enhancer-regulated oncogenes and other lineage-specific factors, which are involved in the maintenance of the disease state | ||||||||||||||||||||
| 体内研究： | BI 894999 is active as monotherapy in AML xenografts, and in addition leads to strongly enhanced antitumor effects in combination with CDK9 inhibitors | ||||||||||||||||||||
| 细胞实验： | Cell lines: MV-4-11B, THP-1, MOLM-13 Concentrations: 10 nM, 100 nM, various concentrations Incubation Time: 4h, 24h, 79 h, 96 h Method: For viability assay, the cells are plated in 96-well flat-bottom microtiter plates and incubated overnight at 37°C in a CO2 incubator. BI 894999 is added at various concentrations for 72 hours or 96 hours. After 6-hour incubation with Alamar Blue solution at 37°C, fluorescence is measured using an excitation wavelength of 531 nm and emission at 595 nm. |
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| 动物实验： | Animal Models: 6-8 week old female NMRI-nude/CIEA-NOG miceDosages: 1 mg/kg, 2 mg/kg, 4 mg/kg, 12 mg/kgAdministration: Oral gavage | ||||||||||||||||||||
| 参考文献： | 1. Daniel Gerlach, 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. 2. Ulrike Tontsch-Grunt, 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. | ||||||||||||||||||||
| 溶解性： | Soluble in DMSO、Ethanol | ||||||||||||||||||||
| 保存条件： | -20℃ | ||||||||||||||||||||
| 配置溶液浓度参考： |
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| 注意： | 部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。 |
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