Molecular Formula | C42H45ClN8O7S |
Molar Mass | 841.37 |
Solubility | DMSO : 100 mg/mL (118.85 mM);H2O : < 0.1 mg/mL (insoluble) |
Storage Condition | -20°C |
In vitro study | dBET6 is a BET bromodegradation agent with high cell permeability. It is effective in most cancer cell lines. dBET6 has a significant degradation effect in cells at concentrations below the nanomolar scale. After cells were treated with 100 nM dBET6 for 1 hour, BRD4 degraded and promoted c-Myc downregulation and induced apoptosis. dBET6 disrupts the overall high efficiency of transcriptional extension, resulting in a large decrease in steady-state mRNA levels. Disruption of the core transcription machinery by BET degradation results in a strong apoptotic response. |
In vivo study | dBET6 was well tolerated. In a diffuse T-ALL mouse model, dBET6 caused a significant reduction in leukemia burden. In addition, dBET6 was administered to mice twice daily (7.5 mg/kg), relative to control mice and mice treated with JQ1(20 mg/kg QD), treatment with dBET6 was beneficial to the survival of the mice. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.189 ml | 5.943 ml | 11.885 ml |
5 mM | 0.238 ml | 1.189 ml | 2.377 ml |
10 mM | 0.119 ml | 0.594 ml | 1.189 ml |
5 mM | 0.024 ml | 0.119 ml | 0.238 ml |