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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)-

, 2334525-50-5, 结构式
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)-
英文别名:
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)-;2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,?]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-(3-{2-[2-(2-{[3-(2,6-dioxopiperidin-3-yl)-4-oxo-3,4-dihydro-1,2,3-benzotriazin-5-yl]amino}ethoxy)ethoxy]ethoxy}phenyl)acetamide
中文名:
中文别名:
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)
安全信息

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

供应商联系电话电子邮件国家产品数优势度
四川省维克奇生物科技有限公司 028-81700200 18116577057 3003855609@qq.com 中国 7887 56
吉林省沃达生物科技有限公司 13504435624 1927928688@qq.com 中国 1382 58
天津普西唐生物医药科技有限公司 010-60605840 15801484223 psaitong@jm-bio.com 中国 29778 58
南京鼎石生物技术有限公司 13501719342 wayne.zheng@elucigenbio.com 中国 4587 58
 

2334525-50-5, 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)- 相关搜索:

  • 对照品
  • C43H43ClN10O7S
  • 2334525-50-5
  • 2-[(9S)-7-(4-chlorophenyl)-4,5,13-trimethyl-3-thia-1,8,11,12-tetraazatricyclo[8.3.0.02,?]trideca-2(6),4,7,10,12-pentaen-9-yl]-N-(3-{2-[2-(2-{[3-(2,6-dioxopiperidin-3-yl)-4-oxo-3,4-dihydro-1,2,3-benzotriazin-5-yl]amino}ethoxy)ethoxy]ethoxy}phenyl)acetamide
  • 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)-
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