2334525-50-5
2334525-50-5 结构式
常见问题列表
生物活性
TD-428 是一种高度特异的 BRD4 降解剂，DC50 为 0.32 nM。TD-428 是一种 BET PROTAC，其中 TD-106 (CRBN 配体) 连接到 JQ1 (BET 抑制剂)，TD-428 可有效诱导 BET 蛋白降解。靶点
|
BRD4 0.32 nM (DC 50 ) |
Cereblon
|
体外研究
TD-428, which comprises TD-106 linked to a BET inhibitor, JQ1 efficiently induce BET protein degradation in the prostate cancer cell line 22Rv1.
TD-428 (0.01-10,000 nM; 72 hours) inhibits the proliferation of 22RV1 cells with a CC
50
of 20.1 nM.
TD-428 (1 nM-10 μM; 12 hours) induces the degradation of BRD4, IKZF1, and IKZF3 proteins.
Cell Cytotoxicity Assay
| Cell Line: | 22RV1 cells |
| Concentration: | 0.01, 0.1, 1, 10, 100, 1000, and 10000 nM |
| Incubation Time: | 72 hours |
| Result: | Inhibited cell proliferation with a CC 50 of 20.1 nM. |
Western Blot Analysis
| Cell Line: | U266 cells |
| Concentration: | 1 nM, 10 nM, 100 nM, 1000 nM, and 10 μM |
| Incubation Time: | 12 hours |
| Result: | Induced the degradation of BRD4, IKZF1, IKZF3 proteins. |