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)-
英文名称: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
分子式:C43H43ClN10O7S
分子量:879.38
EINECS号:
Mol文件: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)- 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)- 用途与合成方法
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。
BRD4 0.32 nM (DC 50 ) |
Cereblon
|
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)-供应商 更多
四川省维克奇生物科技有限公司
联系电话:028-81700200 18116577057
产品介绍:
英文名称:TD-428
CAS:2334525-50-5
纯度:≥98%
包装信息:20mg/10
天津普西唐生物医药科技有限公司
联系电话:010-60605840 15801484223;
产品介绍:
英文名称:TD-428
CAS:2334525-50-5
包装信息:100mg
备注: 试剂级
南京鼎石生物技术有限公司
联系电话: 13501719342
产品介绍:
英文名称: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
CAS:2334525-50-5
纯度:97% LC/GC
包装信息:10mg;25mg;50mg;100mg;250mg;500mg;1g;5g;10g
备注:For research use only