| 产品描述： | NEO2734 (EP31670) 是一种新型的、口服活性的 p300/CBP 和 BET bromodomain 的选择性双重抑制剂，对应的IC50值均<30 nM |
| 靶点： |
p300/CBP(Cell-free assay):<30 nM; BET(Cell-free assay):<30 nM;EpigeneticReaderDomain; HistoneAcetyltransferase |
| 体外研究： |
Treatment of NMC cells with the novel dual p300/CBP and BET bromodomain–selective inhibitor, NEO2734, potently inhibits growth and induces differentiation of NMC cells in vitro; findings that correspond with potentiated transcriptional effects from combined BET and p300 bromodomain inhibition |
| 体内研究： |
In three disseminated NMC xenograft models, NEO2734 provides greater growth inhibition, with tumor regression and significant survival benefit seen in two of three models, compared with a lead clinical BET inhibitor or “standard” chemotherapy |
| 细胞实验： |
Cell lines: NUT carcinoma patient cell lines (TC-797, 14169, 10-15, PER-403) Concentrations: 1 μM Incubation Time: 24 h Method: NUT carcinoma patient cell lines (TC-797, 14169, 10-15, and PER-403) are plated in T-25 flasks and grown in DMEM (797) containing 10 % fetal bovine serum and 1 % penicillin/streptomycin. Cells are treated with either 500 nM OTX-015, 1 μM GNE-781, combination of 62.5 nM GNE-781 and 62.5 nM OTX-015, 1 μM NEO2734, or the equivalent volume of DMSO (0.025 %). At 24H, 2 × 106 cells are spun at 500 × g for 5 minutes at 4 ℃ and washed twice with PBS. Pellets are resuspended in 1 ml of cold PBS and added dropwise while gently vortexing to 9 ml 70 % ethanol in a 15 ml polypropylene centrifuge tube. Fixed cells are then frozen at –20 ℃ overnight. The next day, cells are centrifuged at 500 × g for 10 minutes at 4 ℃ and washed twice with 3 ml of cold PBS. Cells are resuspended in 400 μl of propidium iodide staining solution (0.2 mg/ml RNAse A, 0.02 mg/ml propidium iodide, 0.1 % Triton-X in PB |
| 动物实验： |
Animal Models: tumor bearing NSG mice Dosages: 8 mg/kg Administration: Oral gavage |
| 参考文献： |
1. Chevaun D Morrison-Smith, et al. Combined Targeting of the BRD4-NUT-p300 Axis in NUT Midline Carcinoma by Dual Selective Bromodomain Inhibitor, NEO2734. Mol Cancer Ther. 2020 Jul;19(7):1406-1414. |
| 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。 |
上海工商
危险品化学品经营许可证（不带存储）
营业执照(三证合一)
北京