ChemicalBook CAS数据库列表 6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-
- CAS号:2334525-50-5
- 英文名:6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-
- 中文名:
- CBNumber:CB88249948
- 分子式:C43H43ClN10O7S
- 分子量:879.38
- MOL File:2334525-50-5.mol
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-化学性质
- 密度 :1.50±0.1 g/cm3(Predicted)
- 酸度系数(pKa) :10.70±0.40(Predicted)
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-性质、用途与生产工艺
- 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.
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-上下游产品信息
上游原料
下游产品
6H-Thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine-6-acetamide, 4-(4-chlorophenyl)-N-[3-[2-[2-[2-[[3-(2,6-dioxo-3-piperidinyl)-3,4-dihydro-4-oxo-1,2,3-benzotriazin-5-yl]amino]ethoxy]ethoxy]ethoxy]phenyl]-2,3,9-trimethyl-, (6S)-生产厂家
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