产品说明书
BETd-260
 |
同义名 : | ZBC 260 |
| CAS号 : | 2093388-62-4 | |
| 货号 : | A887929 | |
| 分子式 : | C43H46N10O6 | |
| 纯度 : | 98% | |
| 分子量 : | 798.889 | |
| MDL号 : | MFCD31563593 | |
| 存储条件： |
粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C 液体 -20°C:3-6个月-80°C:12个月 |
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| 溶解度 : |
DMSO: 25 mg/mL(31.29 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 |
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| 动物实验配方： |
| 生物活性 | |||
|---|---|---|---|
| 描述 | PROTAC BET Degrader 23 is a highly potent and efficacious PROTAC targeting on BET with DC50 value of 30pM for degradation of BRD4 in RS4;11 leukemia cell line. PROTAC BET Degrader 23 effectively degraded BRD2, 3 and 4 at concentration of 1nM post 3-hour treatment in RS4;11 cells. A dose-dependent downregulation of c-MYC, a BET target gene, could be observed accompanied with the decreased BET in RS4;11 cells post 24-hour treatment with PROTAC BET Degrader 23 at concentration ranging in 0.03-10nM. PROTAC BET Degrader 23 strongly induced cell cycle arrest in both RS4;11 cell line and MOLM-13 cell line as low as 0.3nM, as well as a robust apoptosis at 3−10 nM concentrations with a 24 h treatment. Administration of PROTAC BET Degrader 23 at dose of 5mg/kg, i.v., every other day, three times a week for 3 weeks, achieved rapid tumor regression with a maximum of >90% regression observed in the xenograft model of human RS4;11 tumor cells[1]. | ||
| 实验方案 | |||
|---|---|---|---|
| 1mg | 5mg | 10mg | |
|
1 mM 5 mM 10 mM |
1.25mL 0.25mL 0.13mL |
6.26mL 1.25mL 0.63mL |
12.52mL 2.50mL 1.25mL |
| 参考文献 |
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